Bacteria constitute a large domain of prokaryoticmicroorganisms. Antibiotics (also called antibacterials) are a type of antimicrobial drug used in the treatment and prevention of bacterial infections, a limited number of antibiotics also possess antiproto
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A novel antitubercular agent that possesses strong inhibitory activity against both Mycobacterium tuberculosis (MIC=0.7-1.5 ug/ml) and some nontuberculosis mycobacteria, inhibits transport activity of MmpL3; also has marked activity against several species of yeasts, including Candida albicans and Cryptococcus neoformans, is also highly efficacious against mycobacteria which show resistance to the most common traditional drugs.
A fourth-generation synthetic fluoroquinolone, broad-spectrum antibacterial agent that is active against both Gram-positive and Gram-negative bacteria; inhibits DNA gyrase and topoisomerase IV.
Relebactam (MK-7655) is a novel β-lactamase inhibitor that inhibited both class A and C β-lactamases in vitro; effectively restored imipenem's activity against imipenem-resistant Pseudomonas and Klebsiella strains at clinically achievable concentrations; reduces imipenem MICs for Enterobacteriaceae with KPC carbapenemases from 16-64 mg/L to 0.12-1 mg/L at a concentration of 4 mg/L.
A potent inhibitor of bacterial enoyl-ACP reductase FabI; demonstrates MICs of 0.015 and 0.008 ug/ml for S. aureus ATCC 29213 and S. aureus ATCC 33592 (MRSA), respectively; demonstrates a Staphylococcus-specific spectrum of activity.
A potent, noncovalent DprE1 inhibitor with IC50 of 43 nM, shows activity against Mycobacterium tuberculosis (Mtb) in vitro with MIC of 0.39 uM.
Macozinone (PBTZ-169, PBTZ169) is a potent, second-generation antituberculosis agent that inhibits DprE1 and displays nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro; PBTZ169 is less cytotoxic than BTZ043 and shows significantly better efficacy at lower concentrations in the murine model of chronic TB, inhibits DprE1 more efficiently than BTZ043.
Sudoterb dihydrchloride is a novel anti-TB agent that has an MIC range of 0.06-0.5 ug/mL..
LL-3858 (Sudoterb;LL3858) is a novel anti-TB agent that has an MIC range of 0.06-0.5 ug/mL..
SIG1459 (SIG-1459) is a novel anti-acne isoprenylcysteine (IPC) small molecule that shows direct antibacterial activity and inhibits TLR2 inflammatory signaling; shows antibacterial activity against C. acnes (MIC= 8.5 uM, MBC =16.1 uM, and MBEC= 12.5 uM), inhibits TLR2 induced IL-8 release from TLR2/TLR2 (IC50= 0.086 uM), TLR2/6 (IC50= 0.209 uM) and IL-1α from TLR2/TLR2 (IC50 =0.050 uM); demonstrates in vivo anti-acne activity.
AgrA inhibitor F19
AgrA inhibitor F19 is a small-molecule AgrA inhibitor that act as antivirulence agent against Gram-positive pathogens, blocks staphylococcal transcription factor AgrA from binding to its promoter and inhibits toxin and virulence factor transcription; binds to C-terminal DNA-binding domain (AgrA_C) from Staphylococcus epidermidis with an affinity of 2.7 uM, potentiates β-lactam antibiotics in a MRSA wound model.
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