Discovery of Indazole Derivatives as a Novel Class of Bacterial Gyrase B Inhibitors.

ABSTRACT: Antibacterials with a novel mechanism of action offer a great opportunity to combat widespread antimicrobial resistance. Bacterial DNA Gyrase is a clinically validated target. Through physiochemical property optimization of a pyrazolopyridone hit, a novel class of GyrB inhibitors were discovered. Guided by structure-based drug design, indazole derivatives with excellent enzymatic and antibacterial activity as well as great animal efficacy were discovered.

SUBMITTER: Zhang J 

PROVIDER: S-EPMC4601062 | biostudies-literature | 2015 Oct

REPOSITORIES: biostudies-literature