Discovery of aminopiperidine based potent & novel topoisomerase inhibitor with broad spectrum anti-bacterial activity.
Jigar DesaiBhaumin PatelNandini PanchalArchana GiteBrijesh DarjiKasinath ViswanathanJinal TrivediPurvi VyasVishwanath PawarPoonam GiriSachchidanand SRajiv SharmaMukul JainPravin IyerSanjay KumarPublished in: Bioorganic & medicinal chemistry letters (2024)
Bacterial DNA gyrase and topoisomerase IV inhibition has emerged as a promising strategy for the cure of infections caused by antibiotic-resistant bacteria. The Novel Bacterial Topoisomerase Inhibitors (NBTIs) bind to a different site from that of the quinolones with novel mechanism of action. This evades the existing target-mediated bacterial resistance associated with quinolones. This article presents our efforts to identify in vitro potent and broad-spectrum antibacterial agent 4l.