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.
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|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4601062 | PMC |
| http://dx.doi.org/10.1021/acsmedchemlett.5b00266 | DOI Listing |
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