2. Academic Validation
  3. Discovery of aminopiperidine based potent & novel topoisomerase inhibitor with broad spectrum anti-bacterial activity

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

Affiliations

  • 1 Zydus Research Centre, Sarkhej Bavla NH No 8A, Moraiya, Ahmedabad 382213, Gujarat, India. Electronic address: jigardesai@zyduslife.com.
  • 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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