Design, synthesis and antitubercular evaluation of novel series of N-[4-(piperazin-1-yl)phenyl]cinnamamide derivatives

• A novel series of 52 N-[4-(piperazin-1-yl)phenyl]cinnamamide derivatives were synthesized.
• The synthesized compounds were evaluated for its antitubercular activity using REMA method.
• Compound 11g with trifluoromethyl substitution showed good antitubercular activity of 3.125 μg/ml.

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 11g 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.

A novel series of 52 N-[4-(piperazin-1-yl)phenyl]cinnamamide derivatives were synthesized and evaluated for its antitubercular activity using REMA method.Figure optionsDownload as PowerPoint slide