Design, in-silico study and biological evaluation of newly synthesized 3-chlorobenzofuran congeners as antitubercular agents

Benzofuran is a heterocyclic scaffold present in various natural products and possess excellent pharmacological properties including anti-tubercular activity as well. A novel series 26 compound containing 3-chlorobenzofuran derivatives are designed, synthesized and spectroscopically characterized. In vitro screening of compounds was done against multidrug resistant Mycobacterium tuberculosis H37Rv strains. Out of these compounds 3a, 3b, 3c, 4b and 4c exhibited excellent inhibitory potency with IC 50 values in the range of 43-104 mu M. Compound 3b was found to be the most potent with IC 50 value of 51.24 mu M and IC 90 value of 88.04 mu M. The compound may serve as lead for future development of potential and effective anti-tubercular agent. (C) 2021 The Author(s). Published by Elsevier B.V.

Automated summary

Benzofuran is a heterocyclic scaffold found in natural products with anti-tubercular activity. A novel series of compounds containing 3-chlorobenzofuran derivatives were designed, synthesized, and screened in vitro, with compound 3b showing the strongest inhibitory potency.