- Novel 1,3,4-thiadiazolium-2-phenylamine chlorides derived from natural piperine as trypanocidal agents: chemical and biological studies.
Novel 1,3,4-thiadiazolium-2-phenylamine chlorides derived from natural piperine as trypanocidal agents: chemical and biological studies.
Bioorganic & medicinal chemistry (2008-01-30)
Welisson da Silva Ferreira, Leonardo Freire-de-Lima, Víctor Barbosa Saraiva, Frederico Alisson-Silva, Lucia Mendonça-Previato, José Osvaldo Previato, Aurea Echevarria, Marco Edilson Freire de Lima
PMID18226906
ABSTRACT
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.