Journal
MEDCHEMCOMM
Volume 9, Issue 8, Pages 1293-1304Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c8md00212f
Keywords
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Funding
- National Science and Technology Major Project of the Ministry of Science and Technology of China [2018ZX09735010, 2017ZX10302301-003-002]
- Chinese Academy of Sciences [154144KYSB20150045, KFZD-SW-207, YJKYYQ20170036]
- National Mega-project of China [2018ZX09721001-003-003]
- Science and Technology Innovation Leader of Guangdong Province [2016TX03R095]
- Guangzhou Science Technology and Innovation Commission [201707010210, 201604020019]
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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 evaluated in vitro against M. tuberculosis strains H37Ra and H37Rv and clinically isolated multidrug-resistant M. tuberculosis strains. Ten compounds displayed minimal inhibitory concentrations (MICs) against M. tuberculosis H37Ra below 2.5 pg mL(-)(1) and 6g was the most active compound (MIC = 0.625 mu g mL(-1)). Compounds 6g and 7a also showed potent inhibitory activity against M. tuberculosis H37Rv (MIC = 0.39 mu g mL(-1)) and several clinically isolated multidrug-resistant M. tuberculosis strains (MIC = 0.39-3.125 mu g mL(-1)). The compounds did not show inhibitory activity against normal Gram-positive and Gram-negative bacteria. They 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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