Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 7, Pages 1997-1999Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.02.022
Keywords
Diamine; Cinnamic acid; Hybridization; Mycobacterium tuberculosis (Mtb); Antimycobacterial activity; Synergy
Categories
Funding
- Department of Biotechnology (DBT), India
- Department of Biotechnology, India [BT/PR7858/Med/14/1142/2006]
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A series of cinnamide derivatives was designed as potential antimycobacterial agents using molecular hybridization approach. The diamine moiety, a key feature of ethambutol and its other analogs, and certain structural features of cerulenin and cinnamic acid were hybridized to obtain cinnamide derivatives. The minimum inhibitory concentration (MIC) of all synthesized compounds was determined against M. tuberculosis H37Rv using Resazurin Microtitre plate Assay (REMA) method. The synthesized molecules showed good to moderate activity with MIC in the range of 5-150 mu M and good safety profile. Additionally, the most potent compound 1a, having MIC 5.1 mu M exhibited synergy with rifampicin. (C) 2011 Elsevier Ltd. All rights reserved.
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