Patel Kavitkumar N, Telvekar Vikas N
Department of Pharmaceutical Sciences & Technology, Institute of Chemical Technology, Matunga (E), Mumbai 400 019, India.
Department of Pharmaceutical Sciences & Technology, Institute of Chemical Technology, Matunga (E), Mumbai 400 019, India.
Eur J Med Chem. 2014 Mar 21;75:43-56. doi: 10.1016/j.ejmech.2014.01.024. Epub 2014 Jan 25.
The analogs of N-[4-(piperazin-1-yl)phenyl]cinnamamide were designed and synthesized by molecular hybridization approach in which part C of the designed molecule was linked through amide and carbamate functionality that improves the physicochemical properties and govern the pharmacokinetic and pharmacodynamic behavior. The systematic modification was done around the Part C to explore the structure activity relationship of antitubercular cinnamamide. All 52 compounds were evaluated for its antitubercular activity against Mycobacterium tuberculosis (M. tb) using Resazurin microtitre plate assay (REMA). Compound 11 g with trifluoromethyl substitution exhibited good antitubercular activity of 3.125 μg/ml. The synthesized N-[4-(piperazin-1-yl)phenyl]cinnamamide derivatives showed promising activity against M. tb.
通过分子杂交方法设计并合成了N-[4-(哌嗪-1-基)苯基]肉桂酰胺类似物，其中设计分子的C部分通过酰胺和氨基甲酸酯官能团连接，这改善了物理化学性质并控制了药代动力学和药效学行为。围绕C部分进行了系统修饰，以探索抗结核肉桂酰胺的构效关系。使用刃天青微量滴定板法（REMA）对所有52种化合物进行了抗结核活性评估，以检测其对结核分枝杆菌（M. tb）的活性。具有三氟甲基取代的化合物11 g表现出良好的抗结核活性，最低抑菌浓度为3.125μg/ml。合成的N-[4-(哌嗪-1-基)苯基]肉桂酰胺衍生物对结核分枝杆菌显示出有前景的活性。
