| DC70585 |
MBX3132 |
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. |
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| DC70587 |
MCB-3681 |
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. |
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| DC70591 |
mCLB073 |
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%. |
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| DC70596 |
MGB-BP-3 |
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). |
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| DC70613 |
MMV688844 |
MMV688844 (MMV844) is a piperidine-4-carboxamide with bactericidal properties against M. abscessus, targets mycobacterial DNA gyrase. |
|
| DC70626 |
Mtb CoaBC inhibitor 1f |
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). |
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| DC70661 |
NPG9 |
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). |
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| DC70717 |
PTC-672 |
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. |
|
| DC70718 |
PTC-847 |
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. |
|
| DC70724 |
Quabodepistat |
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. |
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| DC70725 |
QZN 34 |
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. |
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| DC70750 |
Rv1625c agonist V-59
Featured
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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. |
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| DC70856 |
UAMC-03011 |
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). |
|
| DC70908 |
Xeruborbactam |
Xeruborbactam (QPX7728) is an ultrabroad-spectrum beta-lactamase inhibitor with remarkable activity against a wide range of beta-lactamases, including those that are typically resistant to other inhibitors. |
|
| DC70947 |
G092 |
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. |
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| DC70948 |
GA-O-02 |
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. |
|
| DC70949 |
GA-O-06 |
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. |
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| DC70959 |
6'-Sialyllactose sodium |
6'-Sialyllactose (sodium), a predominant milk oligosaccharide, reduces the internalisation of Pseudomonas aeruginosa in human pneumocytes. |
|
| DC70963 |
CBR-3465 |
CBR-3465 is a mycobacterium tuberculosis (Mtb) type II NADH dehydrogenase inhibitor, with the MIC of 0.16 μM against Mtb. |
|
| DC70964 |
CBR-6672 |
CBR-6672 is a mycobacterium tuberculosis (Mtb) type II NADH dehydrogenase inhibitor, with the MIC of 0.14 μM against Mtb. |
|
| DC70976 |
STC314 |
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. |
|
| DC70981 |
W13 |
W13 is a potent MsbA inhibitor. W13 is an ATPase stimulator with an EC50 of 5.5 µM. |
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| DC71039 |
F-17 |
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. |
|
| DC71071 |
Lactonic sophorolipid |
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. |
|
| DC71091 |
Napyradiomycin A1 |
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. |
|
| DC71121 |
Sulochrin |
Sulochrin is a metabolite produced by Aspergillus terreus var. aureus. I. Sulochrin has antimicrobial activities. |
|
| DC71127 |
Tomopenem |
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. |
|
| DC71203 |
OYYF-175 |
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- |
|
| DC71208 |
G247 |
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. |
|
| DC71258 |
844-TFM |
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. |
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