Discovery of aminopiperidine based potent & novel topoisomerase inhibitor with broad spectrum anti-bacterial activity

  • Bioorg Med Chem Lett. 2024 Oct 1:111:129911. doi: 10.1016/j.bmcl.2024.129911.
Jigar Desai  1 ,  Bhaumin Patel  2 ,  Nandini Panchal  2 ,  Archana Gite  2 ,  Brijesh Darji  2 ,  Kasinath Viswanathan  2 ,  Jinal Trivedi  2 ,  Purvi Vyas  2 ,  Vishwanath Pawar  2 ,  Poonam Giri  2 ,  Sachchidanand S  2 ,  Rajiv Sharma  2 ,  Mukul Jain  2 ,  Pravin Iyer  2 ,  Sanjay Kumar  2
Affiliations
  • 1. Zydus Research Centre, Sarkhej Bavla NH No 8A, Moraiya, Ahmedabad 382213, Gujarat, India. Electronic address: [email protected].
  • 2. Zydus Research Centre, Sarkhej Bavla NH No 8A, Moraiya, Ahmedabad 382213, Gujarat, India.
PMID: 39067715 DOI: 10.1016/j.bmcl.2024.129911
Abstract

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.

Keywords
DNA gyrase; MIC; NBTI; Topoisomerase.
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