| DC49459 |
Antibacterial agent 78 |
Antibacterial agent 78 (compound 30) is an antibacterial agent. |
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| DC49460 |
Ph-Ph+ |
Ph-Ph+ is a hemiprotonic compound, which is produced from phenanthroline (ph) dimerization. Ph-Ph+ has antitumor, antibacterial and antifungal activities. |
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| DC70115 |
2S-alkyne |
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. |
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| DC70120 |
CBR490 |
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). |
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| DC70173 |
ACHN-975 |
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. |
|
| DC70197 |
AN12855 |
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. |
|
| DC70200 |
Antimicrobial peptide BING |
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. |
|
| DC70243 |
BDM88855 Hcl |
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. |
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| DC70244 |
BDM88855 |
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. |
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| DC70258 |
BLI-489 |
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. |
|
| DC70276 |
Burkfloxacin |
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. |
|
| DC70288 |
CBR417 |
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). |
|
| DC70318 |
COR388 |
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. |
|
| DC70319 |
COR588 |
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. |
|
| DC70364 |
DNA gyrase inhibitor EN-7 |
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. |
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| DC70368 |
DU011
Featured
|
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). |
|
| DC70370 |
Durlobactam |
Durlobactam is a novel beta-lactamase inhibitor for treatment of resistant bacterial infections. |
|
| DC70376 |
EC-11716 |
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. |
|
| DC70407 |
FG-944 |
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. |
|
| DC70411 |
FIM1033 |
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. |
|
| DC70424 |
GaMF1 |
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. |
|
| DC70428 |
GC-072 |
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. |
|
| DC70455 |
GSK-229423 |
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. |
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| DC70459 |
GSK3011724A
Featured
|
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. |
|
| DC70470 |
GSK693 |
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. |
|
| DC70521 |
JCP276 |
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. |
|
| DC70555 |
KYT-1 |
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. |
|
| DC70556 |
KYT-36 |
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. |
|
| DC70565 |
LFF-571 |
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. |
|
| DC70570 |
LPXC-516 |
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. |
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