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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 antiprotozoal activity. Together with vaccination, antibiotics have led to the near eradication of diseases such as tuberculosis in the developed world. However, their effectiveness and easy access have also led to their overuse, prompting bacteria to develop resistance.

A bactericidal activity of antibacterials may depend on the bacterial growth phase, and it often requires ongoing metabolic activity and division of bacterial cells. In vitro characterization of antibacterial activity commonly includes the determination of the minimum inhibitory concentration and minimum bactericidal concentration of an antibacterial. To predict clinical outcome, the antimicrobial activity of an antibacterial is usually combined with its pharmacokinetic profile, and several pharmacological parameters are used as markers of drug efficacy.

 
 

Cat. No. Product Name CAS No. Information
PC-35157

Q151

2226449-95-0

Q151 is a highly potent inhibitor of mycobacterium tuberculosis IMPDH2 (MtbIMPDH2) with Kiapp of 18 nM, demonstrates the minimum inhibitory concentrations (MIC) of 1 uM withour significant cytotoxicity.

PC-63299

Bedaquiline fumarate

845533-86-0

Bedaquiline fumarate (R403323, TMC207 fumarate, R207910 fumarate) is a diarylquinoline antibiotic that targets ATP synthase, is effective for the treatment of Mycobacterium tuberculosis infections.

Bacterial Infection

Approved

PC-62613

Nacubactam

2007923-17-1

Nacubactam (OP 0595, RG 6080, RO 7079901) is a diazabicyclooctane that inhibits class A and C β-lactamases with IC50 of <1 uM, also acts as a PBP2-active antibacterial; exhibits MICs of 0.5 to 4 μg/ml for most members of the family Enterobacteriaceae, owing to inhibition of PBP2; has MICs of 1-4 mg/ml for Escherichia coli, Enterobacter, Citrobacter and Klebsiella spp; increases the antibacterial activity of cefepime in both in vitro and in vivo.

Bacterial Infection

Phase 1 Clinical

PC-62249

MAC13772

4871-40-3

MAC13772 is a potent inhibitor of BioA with an IC50 of 250 nM, a novel antibacterial inhibitor that selectively inhibits PABA biosynthesis in M tuberculosis.

PC-61388

Macozinone

1377239-83-2

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.

Bacterial Infection

Phase 2 Clinical

PC-61371

Contezolid

1112968-42-9

Contezolid (MRX I) is an orally active oxazolidinone agent with antibacterial activity Gram-positive pathogens, including MRSA, penicillin-PRSP, PISP, and vancomycin-resistant enterococci (VRE) with MIC of 0.25-4 ug/mL; demonstrates the same or better efficacy than linezolid in both systemic and local infection models against the tested strains.

Bacterial Infection

Phase 3 Clinical

PC-61295

Murepavadin

944252-63-5

Murepavadin (POL7080) is a highly potent, specific, macrocycle Pseudomonas antibiotic for the treatment of bacterial infections caused by Pseudomonas aeruginosa.

Bacterial Infection

Phase 3 Clinical

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