AI Article Synopsis
- A series of cinnamide derivatives were created as potential drugs to fight tuberculosis using a method that combines elements from different chemical compounds.
- These compounds were tested to see how effective they were at inhibiting the growth of Mycobacterium tuberculosis, showing good to moderate activity with MIC values ranging from 5-150 μM.
- The most effective compound, labeled 1a, showed a very low MIC of 5.1 μM and worked well in combination with another antibiotic, rifampicin.
Article 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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| http://dx.doi.org/10.1016/j.bmcl.2011.02.022 | DOI Listing |
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