| Literature DB >> 27476117 |
Remya Ramesh1, Rahul D Shingare1, Vinod Kumar2, Amitesh Anand3, Swetha B4, Sridhar Veeraraghavan5, Srikant Viswanadha5, Ramesh Ummanni6, Rajesh Gokhale3, D Srinivasa Reddy7.
Abstract
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.Entities:
Keywords: BM212; Drug repurposing; MmpL3 inhibitor; Rimonabant; Sila analogue; Tuberculosis
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Year: 2016 PMID： 27476117 DOI： 10.1016/j.ejmech.2016.07.009
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514