piperine and Chagas-Disease

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.

Topics: Alkaloids; Animals; Benzodioxoles; Chagas Disease; Macrophages; Mice; Piperidines; Polyunsaturated Alkamides; Structure-Activity Relationship; Trypanocidal Agents; Trypanosoma cruzi

We describe herein an evaluation of trypanocidal effects of the natural alkaloid piperine and twelve synthetic derivatives against epimastigote and amastigote forms of the protozoan parasite Trypanosoma cruzi, the causative agent of the incurable human disease, Chagas' disease. The results obtained point to piperine as a suitable template for the development of new drugs with trypanocidal activity.

Topics: Alkaloids; Animals; Benzodioxoles; Cells, Cultured; Chagas Disease; Dose-Response Relationship, Drug; Drug-Related Side Effects and Adverse Reactions; Humans; Inhibitory Concentration 50; Parasitic Sensitivity Tests; Piperidines; Polyunsaturated Alkamides; Trypanocidal Agents; Trypanosoma cruzi