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Design, synthesis, and biological evaluation of m-amidophenol derivatives as a new class of antitubercular agents

Abstract

A series of m-amidophenol derivatives (6a-6l, 7a-7q, 9a-9b, 12a-12c, 14 and 15) were designed and synthesized. Their antitubercular activities were also evaluated in vitro against M. tuberculosis H37Ra, H37Rv and clinically isolated multidrug-resistant M. tuberculosis strains. Ten compounds displayed minimal inhibitory concentrations (MICs) against M. tuberculosis H37Ra below 2.5 μg/mL and 6g was the most active compound (MIC = 0.625 μg/mL). The compounds 6g and 7a also showed potent inhibitory activities against M. tuberculosis H37Rv (MIC = 0.39 μg/mL) and several clinically isolated multidrug-resistant M. tuberculosis strains (MIC = 0.39 - 3.125 μg/mL). The compounds did not show inhibitory activity against normal Gram-positive and Gram-negative bacteria. They also exhibited low cytotoxicity against HepG2 and RAW264.7 cell lines. The results demonstrated m-amidophenol as an attractive scaffold for the development of new antitubercular agents.

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Publication details

The article was received on 21 Apr 2018, accepted on 06 Jun 2018 and first published on 07 Jun 2018


Article type: Research Article
DOI: 10.1039/C8MD00212F
Citation: Med. Chem. Commun., 2018, Accepted Manuscript
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    Design, synthesis, and biological evaluation of m-amidophenol derivatives as a new class of antitubercular agents

    N. Zhang, Z. Liu, J. Liang, Y. Tang, L. Qian, Y. Gao, T. Zhang and M. Yan, Med. Chem. Commun., 2018, Accepted Manuscript , DOI: 10.1039/C8MD00212F

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