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Structure–activity relationship studies on 2,5,6-trisubstituted benzimidazoles targeting Mtb-FtsZ as antitubercular agents

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Abstract

Filamenting temperature sensitive protein Z (FtsZ) is an essential bacterial cell division protein and a promising target for the development of new antibacterial therapeutics. As a part of our ongoing SAR studies on 2,5,6-trisubstituted benzimidazoles as antitubercular agents targeting Mtb-FtsZ, a new library of compounds with modifications at the 2 position was designed, synthesized and evaluated for their activity against Mtb-H37Rv. This new library of trisubstituted benzimidazoles exhibited MIC values in the range of 0.004–50 μg mL−1. Compounds 6b, 6c, 20f and 20g showed excellent growth inhibitory activities ranging from 0.004–0.08 μg mL−1. This SAR study has led to the discovery of a remarkably potent compound 20g (MIC 0.0039 μg mL−1; normalized MIC 0.015 μg mL−1). Our 3DQSAR model predicted 20g as the most potent compound in the library.

Graphical abstract: Structure–activity relationship studies on 2,5,6-trisubstituted benzimidazoles targeting Mtb-FtsZ as antitubercular agents

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Article information


Submitted
22 Jul 2020
Accepted
14 Sep 2020
First published
16 Oct 2020

RSC Med. Chem., 2020, Advance Article
Article type
Research Article

Structure–activity relationship studies on 2,5,6-trisubstituted benzimidazoles targeting Mtb-FtsZ as antitubercular agents

K. Haranahalli, S. Tong, S. Kim, M. Awwa, L. Chen, S. E. Knudson, R. A. Slayden, E. Singleton, R. Russo, N. Connell and I. Ojima, RSC Med. Chem., 2020, Advance Article , DOI: 10.1039/D0MD00256A

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