c[Arg-Arg-Arg-Arg-Dip-Dip-Dip] (Compound 8C) shows broad-spectrum activity against drug-resistant Gram-positive and Gram-negative bacteria, with MICs of 3.1, 3,1, 12.5, and 12.5 μg/mL for MRSA (ATCC BAA-1556), S. aureus (ATCC 29213), P. aeruginosa (ATCC 27883), and E. coli (ATCC 25922), respectively.

c[Arg-Arg-Arg-Arg-Nal-Nal-Nal] (Compound 9C) shows broad-spectrum activity against drug-resistant Gram-positive and Gram-negative bacteria, with MICs of 3.1, 3,1, 12.5, and 25 μg/mL for MRSA (ATCC BAA-1556), S. aureus (ATCC 29213), P. aeruginosa (ATCC 27883), and E. coli (ATCC 25922), respectively.

Monocerin is an isocoumarin derivative. Monocerin is isolated from Microdochium bolleyi, an endophytic fungus from Fagonia cretica. Monocerin shows good antifungal, antibacterial, and antialgal activities against Microbotryum violaceum, Escherichia coli, Bacillus megaterium, and Chlorella fusca.

Poly(hexamethylenebiguanide) hydrochloride is an antimicrobial agent, which can be used in medical, apparel, and household textile sectors.

4-Piperidinecarboxamide is a mycobacterial aspartyl-tRNA synthetase (AspS) inhibitor. 4-Piperidinecarboxamide is a promising anti-tuberculosis (TB) agent.

Antibacterial agent 64 is a potent YycG inhibitor (IC50=6.1 µM) and an antibacterial agent. Antibacterial agent 64 combines with ampicillin could synergistically eradicate the biofilm-embedded viable bacteria.

Radicinol is a metabolite of cochliobolus lunata, and absolute stereochemistry of radicinin.

Antibacterial agent 27 is a potent antibacterial compound against Candida species.

Antibacterial agent 26 is a potent antibacterial compound.

Sulfisoxazole acetyl (N1-Acetylsulfisoxazole), a Sulfisoxazole derivative, is an orally active dihydropteroate synthase inhibitor. Sulfisoxazole acetyl has an antibacterial action.

DprE1-IN-1 is a potent, orally active DprE1 inhibitor with favorable hepatocyte stability, low cytotoxicity and low hERG channel inhibition. DprE1-IN-1 displays potent activity against both drug-susceptible and clinically isolated drug-resistant Tuberculosis strains with MICs<0.1 μg/mL, as well as good intracellular antimycobacterial activity with a 1.29 log10 CFU reduction in macrophages.

Anticancer agent 36 (compound 11), a sulfonylurea derivative, is a potent antimicrobial and anticancer agent. Anticancer agent 36 inhibits the microbial growth of B. mycoides, E. coli, and C. albicans with a MIC between 0.156 and 0.039 mg/L. Anticancer agent 36 inhibits A549, PC3 cell growth with IC50s of 19.7 µg/mL, 11.9 µg/mL, respectively.

Antibacterial agent 75 (compound 24) is an antibacterial agent. Antibacterial agent 75 (compound 24) is able to re-sensitize VRSA to vancomycin.

Antibacterial agent 82 (compound 7p) is an antibacterial agent.

Antibacterial agent 76 (compound 9) is an antibacterial agent.

Antibacterial agent 77 (compound 12) is an antibacterial agent.

Antibacterial agent 79 (compound 32) is an antibacterial agent.

Antibacterial agent 80 (compound 20) is an antibacterial agent.

RmlA-IN-2 (Compound 1d) is a potent inhibitor of glucose-1-phosphate thymidylyltransferase (RmlA) with an IC50 of 0.303 μM. RmlA-IN-2 influences monosaccharide l-Rhamnose biosynthetic pathway. RmlA-IN-2 affects bacterial cell wall permeability.

Sulfaguanidine-d4 is the deuterium labeled Sulfaguanidine. Sulfaguanidine, belongs to the class of sulfonamide drug, is an orally active antibiotic. Sulfaguanidine can be used for the research of enteric infections such as bacillary dysentery.

Amp1EP9 is an antimicrobial peptide. Amp1EP9 is a powerful tool for developing potent and nontoxic antimicrobial drugs. Amp1EP9 has the potential for the research of multidrug-resistant bacterial infections.

Antibacterial agent 78 (compound 30) is an antibacterial agent.

Ph-Ph+ is a hemiprotonic compound, which is produced from phenanthroline (ph) dimerization. Ph-Ph+ has antitumor, antibacterial and antifungal activities.

2S-alkyne is an irreversible and clickable inhibitor of Streptococcal pyrogenic exotoxin B (SpeB) with IC50 of 1.4 uM; 2S-alkyne showed irreversible enzyme inhibition in biochemical assays and labeled endogenous SpeB in cultured S. pyogenes supernatants. 2S-alkyne decreased S. pyogenes survival in the presence of human neutrophils and supports the role of SpeB-mediated proteolysis as a mechanism to limit complement-mediated host defense.

90 (CBR-490) is a potent and selective antiwolbachial activity compound (Anti-Wolbachia wMel In vitro HCI cell-based assay IC50=33 nM, IC90=283 nM).CBR490 demonstrates potent antiwolbachial activity was confirmed in L. sigmodontis, Brugia malayi, and Onchocerca ochengi in vivo preclinical models of filarial disease.CBR490 demonbstrated in vitro selectivity against Loa loa (a safety concern in endemic areas).

ACHN-975 (ACHN975) is a potent bacterial LpxC inhibitor with IC50 of 0.68 nM (P. aeruginosa LpxC); ACHN-975 is potent against the P. aeruginosa isolates with MIC50 of 0.06 ug/mL and MIC90 of 0.25 ug/mL. ACHN-975 demonstrated in a neutropenic mouse thigh model with P. aeruginosa ATCC 27853.

AN12855 (AN-12855) is potent, cofactor-independent M. tuberculosis InhA inhibitor, binds to and inhibits InhA with IC50 of 0.03 uM, shows potent activity against whole-cell M. tuberculosis H37Rv with IC90 of 0.09 uM; AN12855 demonstrates potent activity against drug-susceptible and drug-resistant strains of M. tuberculosis, exhibits comparable efficacy to the frontline antitubercular drug isoniazid (INH) in both acute and chronic models of TB infection with a lower potential for resistance development and shows in vitro activity against conventional KatG-mediated INH-resistant M. tuberculosis.

Antimicrobial peptide BING (IRIILRAQGALKI) is a thermostable 13-residue peptide that targets bacterial envelope stress response by suppressing cpxR expression in Gram-negative bacteria.BING downregulates efflux pump components and synergises the effect of antibiotics, and suppresses the development of antibiotic resistance.BING downregulated the expression of efflux pump components mexB, mexY and oprM in P. aeruginosa and significantly synergised the toxicity of antibiotics towards these bacteria.

BDM88855 Hcl is a novel allosteric efflux-pump inhibitor that potentiate antibiotic activity in E. coli through inhibition of its primary RND transporter, AcrAB-TolC.BDM88855 binds to a unique site on the transmembrane domain of the AcrB L protomer, lined by key catalytic residues involved in proton relay, boost antibiotic activity in E. coli by inhibiting the AcrAB-TolC efflux pump.

BDM88855 is a novel allosteric efflux-pump inhibitor that potentiate antibiotic activity in E. coli through inhibition of its primary RND transporter, AcrAB-TolC.BDM88855 binds to a unique site on the transmembrane domain of the AcrB L protomer, lined by key catalytic residues involved in proton relay, boost antibiotic activity in E. coli by inhibiting the AcrAB-TolC efflux pump.

BLI-489 is a bicyclic penem inhibitor that inhibits class A, C, and D beta-lactamases with synergistic effects with piperacillin; The combination of piperacillin-BLI-489 demonstrated improved activity compared to that of piperacillin-tazobactam against the problematic extended-spectrum beta-lactamase- and AmpC-expressing strains.

Burkfloxacin (BFX) is a fluoroquinolone analog that potently inhibits growth of intracellular Burkholderia.Burkfloxacin is active against other gram-negative organisms in vitro, showing similar potency to the widely used fluoroquinolone, ciprofloxacin (Cip), against Escherichia coli ATCC 25922 and Pseudomonas aeruginosa ATCC 27853.Burkfloxacin near-completely inhibits plaque formation by Bt and Bp at concentration of 0.5 uM.Burkfloxacin functions as a canonical fluoroquinolone by inhibiting the negative DNA supercoiling activity of E. coli DNA gyrase.Treatment with Burkfloxacin was significantly more effective than ceftazidime, the current antibiotic of choice, for improving survival and decreasing bacterial counts in major organs in a murine model of fulminant respiratory melioidosis.

CBR417 (CBR-417) is a potent and selective antiwolbachial activity compound (Anti-Wolbachia wMel In vitro HCI cell-based assay IC50=21 nM, IC90=1640 nM).CBR417 demonstrates potent antiwolbachial activity was confirmed in L. sigmodontis, Brugia malayi, and Onchocerca ochengi in vivo preclinical models of filarial disease.CBR417 demonstrates in vitro selectivity against Loa loa (a safety concern in endemic areas).

COR388 (Atuzaginstat) is an orally bioavailable, brain penetrant small-molecule that irreversibly inhibits lysine-gingipain (Kgp, gingipain K) with Ki of <0.01 nM.COR388 blocks the activity of gingipains, a type of toxic protein made by the bacteria Porphyromonas gingivalis ( P. gingivalis ).COR388 reduced the bacterial load of an established P. gingivalis brain infection, blocked Aβ1-42 production, reduced neuroinflammation, and rescued neurons in the hippocampus.

COR588 is a second-generation small-molecule lysine-gingipain (Kgp, gingipain K) inhibitor with novel structure and improved pharmacologic and safety profile prioritized for Alzheimer’s development.

DNA gyrase inhibitor EN-7 (EN-7) is a potent bacterial DNA gyrase inhibitor, is active against pathogenic species that are resistant to ciprofloxacin and other clinically important antibiotics.EN-7 inhibited growth of the wild-type strain (S. aureus) with MIC 1 μM.Strains containing GyrA A34T (mut-3 and mut-9), GyrA P219Q (mut-6), and GyrB K417E (mut-1, mut-2, mut-4, and mut-5) exhibited moderate resistance, with MICs of either 4 or 8 μM.EN-7 inhibited sporulation pathway in the bacterial genus Streptomyces.

DU011 is a noncanonical anti-infective agent and small-molecule inhibitor of capsule biogenesis, targets MprA (Kd=30 nM), a MarR family transcriptional repressor of multidrug efflux pumps, inhibits capsule expression in E. coli. DU011 does not alter Escherichia coli antibiotic resistance and has significantly enhanced inhibition of capsule expression, compared with other proposed MprA ligands, such as salicylate and 2,4-dinitrophenol (DNP).

Durlobactam is a novel beta-lactamase inhibitor for treatment of resistant bacterial infections.

EC-11716 (EC/11716) is a novel mycobacterium tuberculosis gyrase inhibitor with potent anti-tubercular activity (MIC 0.38 uM, M. tuberculosis H37Rv).EC/11716 is active against M. abscessus subspecies and clinical isolates, maintains comparable activity against a panel of clinical isolates covering the M. abscessus complex.EC/11716 is effective against M. abscessus biofilms (MIC 0.78 uM), with better bactericidal activity against biofilms than moxifloxacin.EC/11716 is active against M. abscessus in vivo.

FG944 (FG-944) is a potent selective LpxC inhibitor with MIC50 of 0.5 ug/mL against K.pneumoniae, synergizes with rifampin in carbapenem resistant K. pneumoniae and E. coli.

FIM1033 (FIM-1033) is a potent small-molecule inhibitor of FimH with HAI EC90 of 8 nM, with antibiotica activities, significantly attenuated bacterial loads in pyelonephritis in treated mice.

GaMF1 is a novel antimycobacterial compound that targets the F1FO-ATP synthase γ subunit loop; GaMF1 is bactericidal and is active against multidrug- as well as bedaquiline-resistant strains. Combining GaMF1 with bedaquiline or novel diarylquinoline analogues showed potentiation without inducing genotoxicity or phenotypic changes in a human embryonic stem cell reporter assay. GaMF1 presents an attractive lead for the discovery of a novel class of anti-tuberculosis F-ATP synthase inhibitors.

GC-072 (GC072) is a potent, 4-oxoquinolizine antibiotic with selective inhibitory activity against bacterial topoisomerases (E. coli Topo II/DNA gyrase, IC50=0.18-1.5 uM).GC-072 demonstrated no detectable inhibition of human Topo I and II, is selective for bacterial topoisomerases (IC50>100 uM).GC-072 inhibits E. coli Quinolone-resistant gyrase (IC50=1.3-1.5 uM), S. aureus Gyrase and Topo IV (IC50=2-30 uM).GC-072 demonstrated good activity against B. pseudomallei, with an MIC90 of 0.25 ug/mL.GC-072 exhibited strong in vitro antimicrobial potency against biothreat agents Bacillus anthracis, Yersinia pestis, and Francisella tularensis and category B biothreat agent Burkholderia mallei.GC-072 is efficacious against B. pseudomallei aerosol infection in a mouse model following exposure to a 24-LD50 bacterial challenge.

GSK-229423 is a novel bacterial topoisomerase inhibitor that shows potent inhibition of supercoiling by DNA gyrase from S. aureus with IC50 of 14 nM; displays approximately 70 times more potent against S. aureus DNA gyrase than NXL101; has potent antibacterial activity against a broad spectrum of Gram-positive and Gram-negative bacterial pathogens, including clinical isolates with fluoroquinolone resistance mediated by DNA gyrase and topo IV mutations.

GSK 3011724A (DG-167, GSK-3011724A) is a potent, specific inhibitor of β-ketoacyl-ACP synthase (KasA, Kd=9 nM), shows anti-tubercular activity (MIC H37Rv=0.8 uM); shows much weaker apparent dissociation constant for both Pks10 and Pks (Kd=1.4 uM); inhibits mycolic acid biosynthesis and shows negligible activity against a panel of unrelated proteins and 18 Gram-positive and Gram-negative bacterial species.

GSK693 (GSK-693) is a potent, direct inhibitor of M. tuberculosis enoyl-ACP reductase (InhA) with IC50 of 7 nM, shows equally potent activity against M. tuberculosis H37Rv both intra and extracellularly (MIC=0.2 uM); exhibits activities against multidrug (MDR) and extensively (XDR) drug-resistant clinical isolates as well as in TB murine models when orally dosed.

JCP276 is a novel antibiotic and covalent inhibitor that disrupt M. tuberculosis growth by targeting multiple serine hydrolases.JCP276 is a narrow-spectrum inhibitor of Mycobacterium tuberculosis growth.JCP276 inhibits multiple nonessential serine hydrolases.JCP276 treatment caused accumulation of free lipids and a substantial decrease in lipooligosaccharides, linking SH inhibition to defects in cell envelope biogenesis.

KYT-1 is a potent, selective inhibitor of P. gingivalis virulence factor Arg-gingipain (Rgp) with Ki 40 nM (RgpA/B).KYT-1 showed significant inhibitory effects on SMC proliferation stimulated by Porphyromonas gingivalis.

KYT-36 is a potent, selective, and bioavailable inhibitor of P. gingivalis virulence factor gingipain K (Kgp, lysine-gingipain), potently and selectively inhibits Kgp with Ki of 0.27 nM, respectively.KYT-36 consists of benzyloxycarbonyl (BOC), L-glutaminyl (GLN), methylphenylamino (MPA), L-lysinyl (LYS), and benzylcarbamoyl (BCA) moieties.KYT-36 strongly inhibited degradation of host proteins in culture supernatants and abolished thriving of P. gingivalis in cell cultures and in periodontal pockets in vivo.KYT-36 prevented Kgp-triggered vascular permeability in guinea pigs, i.e. demonstrating its efficacy against bacterial virulence in vivo, with no toxicity effects.

LFF571 is a semisynthetic thiopeptide and bactericidal antibiotic that interferes with bacterial protein synthesis by inhibition of elongation factor EF-Tu, LFF571 is potent in vitro activity against C.difficile strains with MIC90 of 0.25 ug/mL.LFF571 demonstrated activity against most other Gram-positive rods and cocci (MIC50/90, 0.125/0.25 μg/mL) except for bifidobacteria and some species of lactobacilli, showed reduced active activity against Gram-negative anaerobes with MICs for Bacteroides fragilis of 4 and 8 μg/mL.LFF571 inhibits exogenous protein synthesis elongation factor EF-Tu and interferes with the ability for EF-Tu to deliver aminoacylated tRNA to the ribosome.

LPXC-516 is a potent bacterial LpxC inhibitor with IC50 of 0.68 nM (P. aeruginosa LpxC), potent against the P. aeruginosa isolates with MIC90 of 2 ug/mL.

MBX3132 is a small mocule inhibitor of AcrB multidrug efflux pump, fully potentiates the activity of a broad range of antibiotics at 0.1 uM; does not exhibit membrane-disrupting or antibacterial activity.

MCB 3681 is a quinolonyl-oxazolidinone bactericidal antibiotic, has activity in vitro against Gram-positive bacteria. MCB3681 has a potent in vitro activity against C. difficile with MIC90 of 0.064 ug/ml.

mCLB073 (mCLB 073) is a more potent, specific, oral small molecule agonist of the Mtb adenylyl cyclase Rv1625c, an optimized analog of the V-59 for in vivo use.mCLB073 exhibited 17-fold potency improvement against Mtb in cholesterol media relative to V-59 while maintaining excellent pharmacokinetic properties and a good safety profile.mCLB073 (30 mg/kg, oral) reduced Mtb CFUs in the lungs of mice significantly and decreased the extent of lung pathology by 45%.

MGB-BP-3 is a potent bactericidal antibiotic with a completely novel mode of action, selectively binds to the minor grove of microbial DNA, has the potential for Clostridioides difficile infection (CDI).

MMV688844 (MMV844) is a piperidine-4-carboxamide with bactericidal properties against M. abscessus, targets mycobacterial DNA gyrase.

Mtb CoaBC inhibitor 1f is a direct small molecule inhibitor of Mtb 4'-phosphopantothenoyl-l-cysteine synthetase (PPCS, CoaB) domain of the bifunctional Mtb CoaBC (IC50=15.6 uM).Mtb CoaBC inhibitor 1f inhibit CoaBC uncompetitively with respect to 4'-phosphopantothenate, the substrate for the CoaB-catalyzed reaction.Mtb CoaBC inhibitor 1f inhibits Mtb growth in whole-cell activity against Mtb H37Rv (MIC=25.9 uM).

NPG9 (NSR inhibitor NPG9) is a small molecule inhibitor of streptococcus agalactiaenisin resistance protein (NSR) with 58% inhibition at 100 uM (specific growth inhibition assay).

PTC-672 (PTC672) is a novel orally active inhibitor that exhibits a narrow spectrum of activity against Neisseria gonorrhoeae (N. gonorrhoeae, Ng) including MDR isolates (MIC, 0.05 to 0.4 ug/mL), directly inhibits class Ia ribonucleotide reductase (RNR).PTC-672 is inactive against the panel of Gram-negative pathogens and normal gut organism (MICs ranging from 12.5 to ≥62.5 ug/mL).PTC-672 demonstrates clear antibiotic activity preference toward all Neisseria species examined including MDR organisms and the Nm M2092 serogroup B (NMSB) reference strain.PTC-672 targets DNA synthesis and the class Ia RNR large subunit, but not DNA topoisomerases. PTC-672 showed 78% inhibition at 2.5 μM aginst Ng RNR activity, also inhibits Ec RNR, but does not inhibits human RNR at 100 uM.PTC-672 (30 mg/kg) demosntrates in vivo efficacy in a mouse model of gonorrhea.

PTC-847 (PTC847) is a novel orally active inhibitor that exhibits a narrow spectrum of activity against Neisseria gonorrhoeae (N. gonorrhoeae, Ng) including MDR isolates (MIC, 0.05 to 0.1 ug/mL), directly inhibits class Ia ribonucleotide reductase (RNR).PTC-847 is inactive against the panel of Gram-negative pathogens and normal gut organism (MICs ranging from 12.5 to ≥62.5 ug/mL).PTC-847 demonstrates clear antibiotic activity preference toward all Neisseria species examined including MDR organisms and the Nm M2092 serogroup B (NMSB) reference strain.PTC-847 targets DNA synthesis and the class Ia RNR large subunit, but not DNA topoisomerases. PTC-847 showed 93% inhibition aginst Ng RNR activity at 4 uM, also inhibits Ec RNR, but does not inhibits human RNR at 100 uM.

Quabodepistat (OPC-167832) is a highly potent antituberculosis agent with MIC of 0.00024 to 0.002 ug/mL against Mycobacterium tuberculosis, targets DprE1 (IC50=258 nM, recombinant DprE1), an essential enzyme for cell wall biosynthesis.OPC-167832 showed MIC90 of 0.0048 and 0.0027 ug/mL against intracellular M. tuberculosis strains H37Rv and Kurono were 0.0048 and 0.0027, respectively.OPC-167832 showed potent bactericidal activities starting at a dose of 0.625 mg/kg of body weight in a mouse model of chronic TB.OPC-167832 exhibited significant combination effects in 2-drug combinations with delamanid, bedaquiline, or levofloxacin.

QZN 34 is a small molecule pseudomonas aeruginosa PQS quorum-sensing system (PqsR) inhibitor with IC50 of 15 uM, kills planktonic Gram-positives (S. aureus, MIC 6.25 uM) but not Gram-negatives.QZN 34 prevented S. aureus biofilm formation, severely damaged established S. aureus biofilms, and perturbed P. aeruginosa biofilm development.QZN 34 killed planktonic Gram-positive pathogens including S. aureus, Staphylococcus epidermidis, Streptococcus pyogenes, and Clostridioides difficile but not Gram-negative bacteria such as P. aeruginosa and Escherichia. coli.QZN 34 eradicated the mixed-species biofilm against mixed S. aureus and P. aeruginosa biofilms when combined with aminoglycoside.

Rv1625c agonist V-59 (V-59) is a specific small molecule agonist of the Mtb adenylyl cyclase Rv1625c, inhibits Mtb growth in macrophages (EC50=0.3 uM) in an Rv1625c-dependent mechanism.V-59 inhibits Mtb growth in cholesterol media (EC50 0.70 uM), but not in media containing the two-carbon fatty acid acetate, or in standard rich growth media.V-59 stimulates Rv1625c to produce cAMP, which is necessary for V-59 to inhibit Mtb growth.Chemically activating Rv1625c via V-59 preferentially inhibits cholesterol utilization in WT Mtb, rather than equally inhibiting all lipid utilization by the bacterium.

UAMC-03011 is a potent anti-trypanosomal compound (IC50=0.63 uM, T. brucei).UAMC-03011 displays selectivity for Trypanosoma brucei over a panel including Trypanosoma cruzi, L.eishmania infantum, and Plasmodium falciparum (IC50>64 uM).

Xeruborbactam (QPX7728) is an ultrabroad-spectrum beta-lactamase inhibitor, inhibits class A extended-spectrum beta-lactamases with IC50 of 1-3 nM, carbapenemases such as KPC (IC50, 2.9 nM), class C P99 (IC50, 22 nM).QPX7728 displays a remarkably broad spectrum of inhibition, including class B and class D enzymes.QPX7728 is also a potent inhibitor of class D carbapenemases such as OXA-48 from Enterobacteriaceae and OXA enzymes from Acinetobacter baumannii (OXA-23/24/58, IC50 range, 1 to 2 nM) as well as MBLs such as NDM-1 (IC50, 55 ± 25 nM), VIM-1 (IC50, 14 ± 4 nM), and IMP-1 (IC50, 610 ± 70 nM).QPX7728 restored the potency of meropenem against carbapenem-resistant Enterobacterales (CRE), with the meropenem MIC90 decreasing from >64 μg/ml to 0.5 μg/ml for QPX7728 (8 μg/ml).

G092 is a potent inhibitor of MsbA. MsbA is an ABC transporter. Transmembrane ATP-binding cassette (ABC) transporters are crucial cellular machines that move molecules small and large across membranes. G092 has the potential for the research of antimicrobial drugs.

GA-O-02, a 18β-Glycyrrhetinic acid derivative, is a potent antimicrobial and anti-inflammatory agent. GA-O-02 exerts anti-inflammation through the inhibition of NO, pro-inflammatory cytokines and chemokines. GA-O-02 displays a high antimicrobial activity against Gram-positive bacteria.

GA-O-06, a 18β-Glycyrrhetinic acid derivative, is a potent antimicrobial and anti-inflammatory agent. GA-O-06 exerts anti-inflammation through the inhibition of NO, pro-inflammatory cytokines and chemokines. GA-O-06 displays a high antimicrobial activity against Gram-positive bacteria.

6'-Sialyllactose (sodium), a predominant milk oligosaccharide, reduces the internalisation of Pseudomonas aeruginosa in human pneumocytes.

CBR-3465 is a mycobacterium tuberculosis (Mtb) type II NADH dehydrogenase inhibitor, with the MIC of 0.16 μM against Mtb.

CBR-6672 is a mycobacterium tuberculosis (Mtb) type II NADH dehydrogenase inhibitor, with the MIC of 0.14 μM against Mtb.

STC314 is a small polyanion that interact electrostatically with histones. STC314 blocks disruption of lipid-bilayers by histones that inhibits the cytotoxic, platelet-activating and erythrocyte-damaging effects of histones. STC314 has anti-infective effects and can be uesd for sepsis research.

W13 is a potent MsbA inhibitor. W13 is an ATPase stimulator with an EC50 of 5.5 µM.

F-17 is a potential inhibitor of virulence factor. F-17 shows very significant inhibitory effect on biofilm, elastase, pyocyanin, and swarming motility. F-17 also shows a good binding effect on LasR and PqsR. F-17 has no obvious cytotoxicity.

Lactonic sophorolipid is a natural antimicrobial surfactant for oral hygiene. Lactonic sophorolipid, a potential anticancer agent, induces apoptosis in human HepG2 cells through the caspase-3 pathway.

Napyradiomycin A1 is one enantioselective compound of napyradiomycins. napyradiomycins are an intriguing family of halogenated natural products with activity against several tumor cell lines as well as some bacterial strains.

Sulochrin is a metabolite produced by Aspergillus terreus var. aureus. I. Sulochrin has antimicrobial activities.

Tomopenem (CS-023; RO4908463; R-115685) is a longer-half-life parenteral carbapenem. Tomopenem shows broad activity against 63 reference species. The activity of tomopenem against 293 clinical isolates is potent (MIC90, 0.06 to 4 μg/mL). Antianaerobic activity.

OYYF-175, an antimicrobial antifolate, is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 2.36 nM for Escherichia coli DHFR. OYYF-175 exhibits potent broad-

G247 is a specific MsbA inhibitor. G247 acts as a transmembrane domains (TMDs) wedge, symmetrically increasing nucleotide-binding domains (NBDs) separation and preventing conformational transition of MsbA. G247 suppresses ATPase activity by increasing inter-NBD distance.

844-TFM is a NBTI (novel bacterial topoisomerase inhibitor) DNA gyrase inhibitor, with an IC50 of 1.5 μM. 844-TFM exhibits bactericidal properties against M. abscessus.

GSK2556286 (GSK286) is an orally active inhibitor of M. tuberculosis. GSK2556286 inhibits growth within human macrophages (IC50 = 0.07 μM). GSK2556286 is effective against both multidrug-resistant (MDR) or extensively drug-resistant (XDR) and drug-sensitive (DS) M. tuberculosis.

Thaxtomin A is a major phytotoxin produced by S. scabies.

WCK-4234 is a potent β-lactamase inhibitor. WCK-4234 inhibits class A, C, and D β-lactamases activity. WCK-4234 lacks direct antibacterial activity. WCK-4234 potentiates imipenem and meropenem against Enterobacteriaceae with OXA-48/OXA-181 or KPC enzymes, or with combinations of impermeability and AmpC or ESBL activity. WCK-4234 distinctively overcomes resistance mediated by OXA-type carbapenemases.

GSK3036656 (GSK070) is a potent, selective and orally active inhibitor of M. tuberculosis leucyl-tRNA synthetase, with an IC50 of 0.20 μM. GSK3036656 can be used for the research of tuberculosis.

YXL-13 is a potent Pseudomonas aeruginosa (PAO1) inhibitor with an IC50 value of 3.686 μM. YXL-13 can inhibit virulence factors and biofilm formation of PAO1. YXL-13 reduces the pathogenicity and drug resistance of PAO1 by inhibition of the quorum sensing (QS) system. YXL-13 can be used for researching anti-bacteria.

DL-Histidine-15N is a 15N-labeled Pefloxacin.

Sulfametrole is an orally active and potent antibacterial. Sulfametrole can be used for infections research, such as HIV, severe pneumonia and UTIs (urinary tract infections).

Diethylamine NONOate (DEA NONOate, diethylammonium salt) is a nitric oxide donor. Diethylamine NONOate is a potent antimicrobial agent, which can inhibit Escherichia coli growth. Diethylamine NONOate also can enhance preservation of the donor rat heart.

Clorobiocin is a MlaC protein inhibitor that could bind to the MlaC protein. Clorobiocin has antibacterial effects.

N-Butylthiophosphoric triamide (NBPT) is a potent urease inhibitor. Butylthiophosphoric triamide inhibits nitrification and reduces the conversion of urea to NH3 gas.

PC190723 (Compound 2) is an inhibitor of the bacterial cell division protein FtsZ with an IC50 of 55 ng/ml. FtsZ-IN-3 exhibits anti-staphylococcal activity with MIC values of 1 µg/ml for MSSA and MRSA.

CRS3123 (REP-3123) dihydrochloride, a fully synthetic antibacterial agent, potently inhibits methionyl-tRNA synthetase (MetRS) of Clostridioides difficile, inhibiting Clostridioides difficile toxin production and spore formation. CRS3123 dihydrochloride is an oral agent for the research of Clostridioides difficile infection (CDI).

WX-081, an anti-tuberculosis agent, displays excellent anti-mycobacterial activity against M. tuberculosis H37Rv and low cytotoxicity.

PXYC12 is a ribosomal protein S1 (RpsA) antagonist with Kds of 2.67 and 4.67 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of Mycobacterium Tuberculosis (Mtb).

VP-4556 is a potent anti-methicillin-resistant Staphylococcus aureus (MRSA) agent. VP-4556 exhibits significant microbial growth inhibition toward Staphylococcus aureus (ATCC 43300) with MIC of 8 µg/mL. VP-4556 inhibits the growth of methicillin‐resistant Staphylococcus aureus with growth inhibition >95%.

EDA-DA is an unnatural dipeptide building block (an ethynyl-D-alanine and a D-alanine). It incorporates a biorthogonal alkyne group into peptidoglycan (PG) through MurF in the cytoplasmic pathway, which enables selective labeling via a click-chemistry reaction. EDA-DA allows labeling of PG in Gram-positive (B. subtilis), Gram-negative (E. coli and C. trachomatis), Mycobacterium (M. smegmatis) and moss plastids (P. patens) with azide modified fluorescent dyes such as Alexa Fluor 488.

PXYC13 is a ribosomal protein S1 (RpsA) antagonist with Kds of 7.61 and 8.50 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of Mycobacterium Tuberculosis (Mtb).

PXYC2 is a ribosomal protein S1 (RpsA) antagonist with Kds of 6.35 and 5.11 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of Mycobacterium Tuberculosis (Mtb).

PXYC1 is a ribosomal protein S1 (RpsA) antagonist with Kds of 0.81 and 0.31 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of Mycobacterium Tuberculosis (Mtb).

PXYD3 is a ribosomal protein S1 (RpsA) antagonist with Kds of 5.66 and 6.91 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of Mycobacterium Tuberculosis (Mtb).

ADG-2e is a potent antibacterial agent with MICs of 16, 4, 2, and 2 μg/mL for E. coli [KCTC 1682], P. aeruginosa [KCTC 1637], B.subtilis [KCTC 3068], and S. aureus [KCTC 1621], respectively. ADG-2e shows anti-metastatic activity against breast cancer cells.

Tibezonium iodide, an oropharyngeal disinfectant, has antibacterial activity for the prevention of mouth infections.

LA-Bac8c is a Lipoic acid modified antimicrobial peptide with enhanced antimicrobial properties. LA-Bac8c inhibits S. aureus, MRSA, S. epidermidis, E. coli, and P. aeruginosa with MICs of 1, 4, 8, 8, and 8 μg/mL.

VP-4604 is a potent anti-methicillin-resistant Staphylococcus aureus (MRSA) agent. VP-4604 exhibits significant microbial growth inhibition toward Staphylococcus aureus (ATCC 43300) with MIC of 4-8 µg/mL. VP-4604 inhibits the growth of methicillin‐resistant Staphylococcus aureus with growth inhibition >95%.

PXYD4 is a ribosomal protein S1 (RpsA) antagonist with Kds of 3.24 and 1.64 μM for RpsA-CTD and RpsA-CTD Δ438A, respectively. RpsA plays an important role in the trans-translation process of Mycobacterium Tuberculosis (Mtb).

Callophycin A, red seaweed derived metabolite, is potently against C. albicans. Callophycin A exhibits potent activity against drug resistance vaginal candidiasis.

Prussian blue insoluble (Iron(III) ferrocyanide) is a good adsorbent to be used as antidotes for poisoning with cesium or thallium ions. Prussian blue insoluble (Iron(III) ferrocyanide) has anticancerous and antibacterial properties. Prussian blue insoluble (Iron(III) ferrocyanide) can be used as a contrast agent in photoacoustic and magnetic resonance imaging (MRI). Prussian blue insoluble can be used for contrast agents, antidotes and cancer research.

Methicillin sodium hydrate is a narrow-spectrum β-lactam antibiotic, acts by inhibiting penicillin-binding proteins (PBPs). Methicillin sodium hydrate is active against Staphylococcus aureus and Staphylococcus epidermidis that are resistant to other penicillins. Methicillin sodium hydrate can be used for the research of skin infections, osteomyelitis, and endocarditis.

3-Chlorogentisyl alcohol is a potent E. coli β-glucuronidase inhibitor with an IC50 value of 0.74 µM, an Ki value of 0.58 µM. 3-Chlorogentisyl alcohol shows antiproliferative activity. 3-Chlorogentisyl alcohol has the potential for the research of anti-cancer and anti-inflammatory therapies.

Alpibectir is an antibacterial agent.

ANT3310 sodium is a broad-spectrum covalent Serine β-Lactamase inhibitor, with IC50 values ranging from 1 nM to 175 nM (a panel of Serine β-Lactamase). ANT3310 sodium potentiates activity of β-lactam antibiotics against Carbapenem-Resistant Enterobacterales (CRE) and Acinetobacter baumannii (CRAB). ANT3310 sodium can be used in the research of bacterial infection.

BPH-1086 (compound 10) is an IspH inhibitor, IspH domain fused with ribosomal protein S1 (RPS1) can bind to mRNA or form part of the bacterial ribosome.

UNC10201652 is a potent Loop 1 (L1)-specific gut bacterial β-glucuronidase (GUSs) inhibitor with an IC50 value of 0.117 μM for E. coli GUS. UNC10201652 can block SN-38 glucuronide processing only in individuals whose fecal gut microbiota is highly abundant in L1 GUS enzymes.

Avibactam sodium (NXL-104) dihydrate is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively.

Penamecillin (Wy 20788) an acetoxymethyl ester of Penicillin G. Penamecillin is an orally active antibacterial agent.

Nifurtoinol is a nitrofuran-derivative antibiotic with antibacterial effects. Nifurtoinol can be used for the research of urinary tract infections.

MRV03-037 is a selective colibactin-activated peptidase (ClbP) inhibitor that blocks the genotoxic effect of Colibactin on eukaryotic cells. MRV03-037 prevents gut bacterial genotoxin production.

Azidocillin, a semi-synthetic Penicillin, is an orally active β-lactam antibiotic. Azidocillin bears an azide functionality and retains on-target activity within bacteria. Azidocillin can be used to research osteitis caused by dental surgery, otitis media, enterococcal septicemia and other bacterial infectious diseases.

(R)-(-)-α-Phellandrene ((-)-α-Phellandrene) is an the (R)-(-)-stereoisomer of α-phellandrene. α-phellandrene is an orally active cyclic monoterpene that attenuates inflammatory response, and induces DNA damage.

Megazol is an orally active antibacterial agent. Megazol has effective inhibitory against T. b. brueei with an EC50 of 0.01 μg/mL. Megazol can be used for the research of protozoan infections.

Cefroxadine (CGP 9000) is an orally active cephalosporin antibiotic. Cefroxadine is more effective than cephalexin against Escherichia coli and Klebsiella pneumoniae with MIC values of 3.13 and 1.56 μg/mL respectively with a concentration of 106 μg/mL. Cefroxadine can be used for the research of infection.

Olanexidine is an antibacterial agent. Olanexidine is active against a wide range of bacteria, imcluding both Gram-positive and Gram-negative bacteria Olanexidine is also an antiseptic. Olanexidine can be used in the research of infection and inflammation.

TH-Z145, a lipophilic bisphosphonate, is a FPPS inhibitor (IC50: 210 nM).

Cyclacillin (Wy-4508) is an orally active aminopenicillin antibiotic, shows antibacterial activity against a wide range of gram-positive and gram-negative pathogens.

Octenidine is a potent antibacterial agent, possessing activity against multidrug-resistant Gram-negative pathogens. Octenidine can inhibit the expression of biofilm genes and destroy the formation of biofilms.

GE 2270A (MDL 62879) is an antibiotic. GE 2270A inhibits gram-positive bacteria and anaerobes by inhibiting protein synthesis. GE 2270A can be used for the research of infection.

Gallichrome is an active peptide. Gallichrome can interact directly with the hydroxamate moieties of the siderophore. Gallichrome can be used for the research of the uptake of iron in many gram-positive and gramnegative bacteria.

MRV03-070 is an inhibitor of colibactin-activating peptidase ClbP with an IC50 value of 69 nM, acts like biosynthetic precursor precolibactin.

PNU-101603 is a metabolite of Sutezolid. PNU-101603 has excellent activity against Mycobacterium tuberculosis (MTB).

Cefilavancin (TD-1792) is a potent multivalent glycopeptide-cephalosporin heterodimer antibiotic with effective activity against Gram-positive bacteria. Cefilavancin has been used to research skin infections.

Pexiganan (MSI 78 free base) is a synthetic analog of magainin 2. Pexiganan is a potent and orally active broad-spectrum antimicrobial peptide. Pexiganan can be used in the research of infections, such as diabetic foot ulcer infections.

Bio-AMS (TFA) is a potent bacterial biotin protein ligase inhibitor. Bio-AMS (TFA) possesses selective activity against Mycobacterium tuberculosis (Mtb) and arrests fatty acid and lipid biosynthesis.

MK-3402 is a metallo-beta-lactamase inhibitor (Example 303 in reference patent). MK-3402can be used in the research of bacteria.

Bischloroanthrabenzoxocinone is a potent Type II fatty acid synthesis (FASII) inhibitor. Bischloroanthrabenzoxocinone inhibits fatty acid synthesis. Bischloroanthrabenzoxocinone shows antibacterial activities and inhibits phospholipid, DNA, RNA, protein, and cell wall synthesis.

4-Hydroxyoxyphenbutazone kills both replicating and nonreplicating (NR) Mycobacterium tuberculosis (Mtb), including Mtb resistant to standard drugs. 4-Hydroxyoxyphenbutazone is a potent inhibitor of cytokine production. 4-Hydroxyoxyphenbutazone is an immunosuppressive drug and has the potential for rheumatoid arthritis research.

Fusafungine (Bioparox; Fusaloyos; Locabiotal) is a potent and orally active antibiotic and anti-inflammatory agent. Fusafungine has the potential for the research of upper respiratory airways disease (URAD).

Almurtide (nor-MDP), a muramyl dipeptide derivative with anti-inflammatory and anti-tumor activity. Almurtide also shows protective effects against intraperitoneal Pseudomonas aeruginosa infection or intravenously Candida albicans infection in mice. Almurtide also inhibits the carcinogenic Friend leukemia virus.

Duramycin (Moli1901) is a lantibiotic derived from Streptomyces cinnamoneuma. Duramycin also is a antimicrobial peptide. Duramycin can be used for the research of cystic fibrosis (CF).

Cymal-6 (Cyclohexyl-hexyl-β-D-maltoside) is a potent TEM-1 beta-lactamase inhibitor with an Ki value of 40.05 µM. Cymal-6 (Cyclohexyl-hexyl-β-D-maltoside) can be used as glycosidic surfactant.

Lipid X is a novel monosaccharide precursor of Lipid A (the active moiety of gram-negative endotoxin). Lipid X is protective against endotoxin administered to mice and sheep and against life-threatening gram-negative infections in mice.

MMV676584 has anti-tuberculosis avtivity. MMV676584 is a novel drug candidate for eumycetoma.

EBL-3183, an indole-2-carboxylate, is a potent metallo-β-lactamase (MBL) inhibitor. EBL-3183 is reversibly binding, non-covalent, competitive NDM-1 inhibitor with a pIC50 of 7.7.

B746 is a clofazimine analog with anti-Mycobacterium avium complex (MAC) activity and is less effective when used with clofazimine or streptomycin.

AM4085 is a potent, orally bioavailable lectin domain of FmLH antagonist with IC50 of 0.19 uM.

BB2-50F is a bactericidal inhibitor of M. tuberculosis with MIC value of 8 uM (H37Rv), inhibits succinate dehydrogenase and the F1Fo-ATP synthase.

BDM71339 is the first small molecule inhibitor of mycobacterial transcriptional regulator EthR, boosts ten times the activity of ethionamide in TB-infected macrophages at low nanomolar concentrations (EC50=72 nM) in vitro.

BDM88855 Hcl is a novel allosteric efflux-pump inhibitor that potentiate antibiotic activity in E. coli through inhibition of its primary RND transporter, AcrAB-TolC.

BDM91288 is a pyridylpiperazine-based AcrB efflux pump inhibitor, potentiate the activity of a panel of antibiotics against K. pneumoniae.

BFA1 is a specific small-molecule activator of Burkholderia FixLJ signaling pathway, inhibit the virulence of multiple pathogenic Burkholderia species.

COE2-2hexyl is a broad-spectrum antibacterial conjugated oligoelectrolyte (COE), does not evoke bacterial resistance, inhibits methicillin-resistant S. aureus (MRSA, MT3302) with MIC of 1 ug/mL.

Cresomycin (CRM) is a bridged macrobicyclic antibiotic via inhibiting bacterial ribosome, shows broad efficacy of CRM against clinical isolates of MDR Gram-negative pathogens differentiates the synthetic macrobicyclic class from traditional lincosamides.

CUO246 (CUO-246) is a potent, selective bacterial DNA gyrase/topoisomerase IV inhibitor, CUO246 is active in vitro against a broad range of Gram-positive, fastidious Gram-negative, and atypical bacterial pathogens.

D66 is a specific small molecule that disrupts S. Typhimurium membrane voltage without cell lysis, prevents S. Typhimurium survival in macrophages (IC50=6.0 uM) and inhibits bacterial growth under conditions that compromise the cell envelope.

DS01750413 is a novel FtsZ inhibitor and new derivative of PC190723 (Cat. PC-47012), inhibits S. aureus FtsZ protein with IC50 of 2 mg/L, has an IC50 of 0.03 mg/L in cell elongation assay of B. subtilis.

EPM35 (Efflux pump modulator 35) is a small molecule that bind AcrB (KD=0.29 uM), inhibit AcrAB-TolC and modulates bacterial efflux pump activity, reduces bacterial intracellular load.

GSK030 (GSK3212030A) is an antimalarial compound that targets blood-stage activity of the Plasmodium falciparum and Plasmodium vivax parasites.

GSK147 (GSK-147) is an antimalarial compound that targets blood-stage activity of the Plasmodium falciparum and Plasmodium vivax parasites (Pf IC50=40 nM).

GSK692 (GSK-692) is an antimalarial compound that targets blood-stage activity of the Plasmodium falciparum and Plasmodium vivax parasites (Pf IC50=10 nM).

HR3744 is a selective small molecule inhibitor of S. aureus exoprotein expression regulator (SaeR) withEC50 of 10 uM in saeP1 promoter assays, reduces expression of hla and other virulence factors.

HSGN-189 is a potent lipoteichoic acid (LTA) biosynthesis inhibitor, exhibits potent antibacterial activity against both MRSA and VRE strains with MICs of 1 ug/mL.

IITR06144 is a novel nitrofuran and exhibits broad-spectrum bactericidal activity against most MDR bacteria (MIC, 0.5 mg/mL).

JBD1 is a small molecule compound that strongly inhibits biofilm formation of S. aureus, including methicillin-resistant strains, induces biofilm inhibition and metabolic remodeling through respiratory activation.

JMV7061 (JMV-7061) is a novel potent, selective bacterial metallo-β-lactamase (MBL) inhibitor, shows submicromolar activities against VIM-type enzymes and strong NDM-1 inhibition (Ki=10-30 nM).

JSF-2414 (JSF2414) is a potent, small molecule GyrB/ParE dual binding inhibitor, simultaneously binds to ATP binding regions of DNA gyrase (GyrB) and topoisomerase (ParE) and displays potent in vitro activity against strains of MRSA, VRSA and VISA.

JSF-2659 is the orally bioavailable, phosphate prodrug of JSF-2414, JSF-2659 (100 and 1 g/kg, p.o.) is highly efficacious in reducing microbial burdens in animal models of Neisseria gonorrhoeae vaginal infection as well as VRSA and C. difficile-induced co

JSF-3269 is a small molecule antibacterial inhibitor against Enterococcus faecium with MIC of 1.9-3.8 uM and minimal bactericidal concentration (MBC) of 7.7-15 uM.

JSF-3285 (JSF3285) is a potent small molecule inhibitor of the M. tuberculosis β-ketoacyl synthase KasA with Kd of 70.7 nM in MST assays, shows activity against H37Rv strain with MIC 0.2 uM.

KKL-55 is a specific small molecule inhibitor of bacterial trans-translation by binding to longation factor thermo-unstable (EF-Tu, Kd=2 uM), inhibits binding between EF-Tu and tmRNA but not between EF-Tu and tRNA, has broad-spectrum antibiotic activity.

KSK67 is a potent small molecule inhibitor of bacterial transcriptional activator PrfA with IC50 of 67 nM, reduces virulence factor expression in L. monocytogene.

LPC-233 (LPC233) is a highly potent and specific inhibitor of UDP-3-O-(R-3-hydroxyacyl)-N-acetylglucosamine deacetylase LpxC (Ki=8.9 pM), specifically inhibits lipid A synthesis and displays outstanding antibiotic activities.

MD-124 is a potent antibiotic adjuvant against Gram-negative bacteria, sensitizes various Gram-negative bacterial species and strains, including multidrug resistant pathogens, toward existing antibiotics.

MMV1091186 (MMV 1091186) is an antimalarial compound that inhibit P. falciparum cytoplasmic isoleucyl tRNA synthetase (cIRS) with IC50 of 0.87 uM.

MMV652103 is an antimalarial imidazopyridazine compound, exerts potent and selective cytotoxicity in ER+ breast cancer cells, potently inhibits the oncogenic PI4KB and PIK3C2G lipid kinases with IC50 of 1.7 and 0.085 uM, respectively.

MSU-43085 is a potent, orally bioavailable inhibitor of Mycobacterium tuberculosis (Mtb, EC50=120 nM) and M. abscessus survival, targets MmpL3.

ND-011992 is a cytochrome bd oxidase (Cyt-bd) inhibitor, inhibits Mycobacterium tuberculosis respiratory complex I with IC50 of 0.12 uM, targets respiratory complex I and bo3 oxidase in addition to bd-I and bd-II oxidases.

NSC116565 is a potent, time-dependent inhibitor of Mycobacterium tuberculosis (M.tb) ketol-acid reductoisomerase (KARI) with Ki of 95.4 nM.

NTB-3119 (NTB3119) is a novel benzothiopyranone derivative and anti-tuberculosis agent with potent in vitro activity against both drug-susceptible and drug-resistant tuberculosis clinical strains.

OTB-658 (OTB658) is a novel oxazolidinone anti-tuberculosis agent, shows potent antibacterial activity against Mycobacterium tuberculosis, especially multi-drug resistant tuberculosis (MDR-TB) in vitro and in vivo.

PKZ18-22 is a potency improved analog of PKZ18, inhibitiong tRNA-regulated gene expression of gram-positive bacteria, shows MIC value of 8 ug/mL against S. aureus.

SAV13 is a selective small molecule inhibitor of S. aureus exoprotein expression regulator (SaeR) withEC50 of 1.06 uM in luciferase assays, reduces expression of hla and other virulence factors.

Savirin (S. aureus virulence inhibitor) is a small molecule inhibitor inhibiting agr quorum sensing in S. aureus by blocking the transcriptional function of AgrA.

SF235 is a small-molecule inhibitor of macrophage infectivity potentiator (Mip) protein with IC50 and Ki 0.42 and 0.29 uM against B. pseudomallei Mip (BpMip) peptidyl-prolyl cis/trans isomerase (PPIase) activity, reduce B. pseudomallei virulence in vitro.

SK-017154-O is a specific and noncompetitive inhibitor of PelA, specifically inhibits PelA esterase activity with IC50 of 11 uM, inhibits Pel-dependent PA14 biofilms with IC50 of 1.8 uM.

SMARt751 is a small molecule that interacts with the transcriptional regulator VirS of M. tuberculosis, up-regulates expression of the mymA operon, reverses resistance to ethionamide both in vitro and in vivo.

SMT-738 is a small-molecule inhibitor of bacterial lipoprotein transport complex (LolCDE), shows potent and highly selective antimicrobial activity.

TBAJ-5307 is a broad spectrum anti-non-tuberculous mycobacteria (NTM) inhibitor targeting FO-domain of F1FO-ATP synthase, shows MIC50 of 4.5 nM and 6 nM against the Mab subsp. abscessus smooth strain and rough strain respectively.

TBI-166 is a potential next-generation antituberculosis riminophenazine with activity against Mycobacterium tuberculosis (0.063  μg/ml).

TPP8 is a small molecule antibacterial inhibiting the ATPase of DNA gyrase with IC50 of 0.3 uM, binds and inhibits the ATPase domain of the gyrase B subunit, shows activity against M. abscessus strains with MIC of 0.04-0.2 uM.

TXA707 is the active metabolite of TXA709 and bacterial protein FtsZ inhibitor, maintains potent activity against S. aureus strains (e.g., MRSA, VRSA, DNSSA, and LNSSA) that are resistant to current SOC antibiotics.

TXA709 is a prodrug of FtsZ-targeting benzamide compound (TXA707) with enhanced metabolic stability, demonstrates improved pharmacokinetic properties, and superior in vivo antistaphylococcal efficacy (both oral and intravenous) relative to previously iden

TXY436 is an N-Mannich base derivative and FtsZ-directed prodrug of PC190723, TXY436 is effective against S. aureus can also target Gram-negative bacteria, such as Escherichia coli.

TXY541 is a 1-methylpiperidine-4-carboxamide prodrug of PC190723 and bacterial protein FtsZ inhibitor, TXY541 is efficacious in vivo in mouse models of systemic infection with both methicillin-sensitive and methicillin-resistant S. aureus.

VU0026921 is a small molecule modulator of metal homeostasis in gram-positive pathogens, disrupts metal homeostasis in multiple Gram-positive bacteria, leading to increased reactive oxygen species and cell death.