Novel 1,3,4-thiadiazolium-2-phenylamine chlorides derived from natural piperine as trypanocidal agents: Chemical and biological studies

We herein describe the synthesis and characterization of nine new 1,3,4-thiadiazolium-2-phenylamine chlorides derived from natural piperine. We evaluate their toxic effects against the different evolutive forms of Trypanosoma cruzi, and the host cell (murine macrophages). The results obtained show that mesoionic hydrochloride MI possesses the best activity profile. Compound MI may be a prototype for use in the development of a new chemotherapeutic agent with high efficiency, which may be employed in the treatment of Chagas’ disease.

Synthesis and evaluation of trypanocidal activity of nine new 1,3,4-thiadiazolium-2-phenylamine chlorides derived from natural amide piperine are reported. Among them MI showed potent trypanocidal activity with reduced toxicity to macrophages.Figure optionsDownload as PowerPoint slide