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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 Information
PC-49547

JMV-7061

Metallo-β-lactamase inhibitor

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).
PC-49514

TBA-7371

DprE1 inhibitor

TBA-7371 (TBA7371, AZ 7371) is a potent, non-covalent inhibitor of decaprenylphosphoryl-β-D-ribose 2'-epimerase (DprE1) with IC50 of 10 nM, an enzyme involved in mycobacterial cell wall biogenesis.
PC-49388

MRV03-069

ClbP inhibitor

MRV03-069 is a small molecule compound that potently and specifically inhibit the colibactin-activating peptidase ClbP (IC50=28 nM), inhibits colibactin-associated genotoxicity.
PC-49326

TPP8

DNA Gyrase inhibitor

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.
PC-49315

Fabimycin

FabI inhibitor

Fabimycin is a potent, specific inhibitor of the enoyl-acyl carrier protein reductase enzyme FabI, exhibits impressive activity against >200 clinical isolates of Escherichia coli, Klebsiella pneumoniae (MIC, 1 ug/mL), and Acinetobacter baumannii, and does not kill commensal bacteria.
PC-49257

JSF-2659

GyrB/ParE inhibitor

JSF-2659 is the orally bioavailable, phosphate prodrug of JSF-2414, JSF-2659 (100 and 250 mg/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 colitis models.
PC-49256

JSF-2414

GyrB/ParE inhibitor

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.
PC-49186

SF235

Mip inhibitor

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.
PC-49180

BDM71339

EthR inhibitor

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.
PC-49179

BVL-GSK098

M.tb VirS inhibitor

BVL-GSK098 (Alpibectir) is a small molecule able to inhibit Mycobacterium tuberculosis transcription regulator VirS, boosts bioactivation of ethionamide (ETH) and lower ETH MIC.
PC-49166

TXA707

FtsZ inhibitor

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.
PC-49165

TXY541

FtsZ inhibitor

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.

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