Synthesis and preliminary biological evaluation of novel N-(3-aryl-1,2,4-triazol-5-yl) cinnamamide derivatives as potential antimycobacterial agents: An operational Topliss Tree approach

A series of novel N-(3-aryl-1,2,4-triazol-5-yl) cinnamamide derivatives were designed on basis of structural similarity to the known FAS II inhibitors. Topliss operational method was used to optimize the potency of molecules. The minimum inhibitory concentration (MIC) of all synthesized compounds was determined against Mycobacterium tuberculosis H37Rv using resazurin microtitre assay (REMA) plate method. The synthesized compounds exhibit antimycobacterial activity in the range of 5–95 μM with a good safety profile.

Graphical abstractA novel series of N-(3-aryl-1,2,4-triazol-5-yl) cinnamamide derivatives were synthesized as potential antimycobacterial agents. Topliss operational method was used successfully to optimize the molecules with regards to activity and significant improvement was observed from >90 μM to <5 μM against Mycobacterium tuberculosis H37Rv.Figure optionsDownload full-size imageDownload as PowerPoint slide