학술논문
Structure–activity relationship studies on 2,5,6-trisubstituted benzimidazoles targeting Mtb-FtsZ as antitubercular agentsElectronic supplementary information (ESI) available: Synthetic procedures and characterization data for all key synthetic intermediates; 1H and 13C NMR spectra of all new 2,5,6-trisubstituted benzimidazoles. See DOI: 10.1039/d0md00256a
Document Type
Article
Author
Source
MedChemComm; 2021, Vol. 12 Issue: 1 p78-94, 17p
Subject
Language
ISSN
20402503; 20402511
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, 20fand 20gshowed 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 20gas the most potent compound in the library.