期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 122, 期 -, 页码 723-730出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.07.009
关键词
Drug repurposing; Tuberculosis; Rimonabant; BM212; Sila analogue; MmpL3 inhibitor
资金
- CSIR, New Delhi [HCP001, BSC-0124]
- UGC, New Delhi
- CSIR, New Delhi
The structural similarity between an MmpL3 inhibitor BM212, and a cannabinoid receptor modulator rimonabant, prompted us to investigate the anti-tubercular activity of rimonabant and its analogues. Further optimization, particularly through incorporation of silicon into the scaffold, resulted in new compounds with significant improvement in anti-tubercular activity against Mycobacterium tuberculosis (H37Rv). The sila analogue 18a was found to be the most potent antimycobacterial compound (MIC, 31 ng/mL) from this series with an excellent selectivity index. (C) 2016 Elsevier Masson SAS. All rights reserved.
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