Design, synthesis, in vitro and in silico studies of 2, 3-diaryl benzofuran derivatives as antitubercular agents.

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ID: 106040
2020
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Abstract
As a part of our drug discovery program for anti-tubercular agents, a total of seventeen 2, 3-diaryl benzofuran hybrids were designed, synthesized and screened for their anti-tubercular potential against Mycobacterium tuberculosis H37Ra avirulent strain. Out of seventeen, four derivatives showed significant activity against M. tuberculosis H37Ra avirulent strain (ATCC 25177) with MIC value ranging from 12.5 to 50 µg/mL but out of four, one derivative (9E) was significantly active (MIC 12.5 μg/mL), which was further supported by the molecular docking energy (-8.4 kcal/mol) with respect to the first line anti-tubercular drug, isoniazid (-6.2 kcal/mol) on the target Polyketide Synthase-13. All the derivatives were also evaluated for their cytotoxicity against the normal lung cell line L-132 by the MTT assay and no toxicity was observed up to 27.4 µg/mL concentration. This report on the antitubercular potential of benzofuran derivatives may be of great help in anti-tubercular drug development.
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bhukya2020designbioorganic Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Bhukya, Balakishan;Shukla, Aparna;Chaturvedi, Vinita;Trivedi, Priyanka;Kumar, Shailesh;Khan, Feroz;Negi, Arvind S;Srivastava, Santosh Kumar;
Journal Bioorganic chemistry
Year 2020
DOI
S0045-2068(20)30076-6
URL
Keywords
benzofuran anti-tubercular activity in-silico studies semi-synthetic derivatives

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