肉桂酰胺衍生物的设计、合成及抗分枝杆菌活性：一种分子杂交方法。
Design, synthesis and antimycobacterial activity of cinnamide derivatives: a molecular hybridization approach.
机构信息
Department of Pharmaceutical Sciences & Technology, Institute of Chemical Technology, NP Marg, Matunga, Mumbai 400 019, India.
出版信息
Bioorg Med Chem Lett. 2011 Apr 1;21(7):1997-9. doi: 10.1016/j.bmcl.2011.02.022. Epub 2011 Feb 12.
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.
设计了一系列肉桂酰胺衍生物作为潜在的抗分枝杆菌药物，采用分子杂交方法。乙胺丁醇及其类似物的关键特征二胺部分和苍耳素及肉桂酸的某些结构特征被杂交以获得肉桂酰胺衍生物。使用 Resazurin 微量板测定法（REMA）测定所有合成化合物对结核分枝杆菌 H（37）R（v）的最低抑菌浓度（MIC）。合成的分子表现出良好至中等的活性，MIC 范围为 5-150 μM，安全性良好。此外，具有 MIC 5.1 μM 的最有效化合物 1a 与利福平表现出协同作用。
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