Structure-activity relationship studies on 2,5,6-trisubstituted benzimidazoles targeting -FtsZ as antitubercular agents.
Journal:
RSC medicinal chemistry
Published Date:
Oct 16, 2020
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 -FtsZ, a new library of compounds with modifications at the 2 position was designed, synthesized and evaluated for their activity against -H37Rv. This new library of trisubstituted benzimidazoles exhibited MIC values in the range of 0.004-50 μg mL. Compounds , , and showed excellent growth inhibitory activities ranging from 0.004-0.08 μg mL. This SAR study has led to the discovery of a remarkably potent compound (MIC 0.0039 μg mL; normalized MIC 0.015 μg mL). Our 3DQSAR model predicted as the most potent compound in the library.
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