Design, synthesis and antimycobacterial activity of cinnamide derivatives: a molecular hybridization approach

Bioorg Med Chem Lett. 2011 Apr 1;21(7):1997-9. doi: 10.1016/j.bmcl.2011.02.022.

Manoj D Kakwani ¹, Prashant Suryavanshi, Muktikant Ray, M G R Rajan, Sharmila Majee, Abdul Samad, Padma Devarajan, Mariam S Degani

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Affiliation

1 Department of Pharmaceutical Sciences & Technology, Institute of Chemical Technology, NP Marg, Matunga, Mumbai 400 019, India.

PMID: 21376586 DOI: 10.1016/j.bmcl.2011.02.022

Abstract

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 H(37)R(v) using Resazurin Microtitre plate Assay (REMA) method. The synthesized molecules showed good to moderate activity with MIC in the range of 5-150 μM and good safety profile. Additionally, the most potent compound 1a, having MIC 5.1 μM exhibited synergy with rifampicin.

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