da Silva Ferreira Welisson, Freire-de-Lima Leonardo, Saraiva Víctor Barbosa, Alisson-Silva Frederico, Mendonça-Previato Lucia, Previato José Osvaldo, Echevarria Aurea, de Lima Marco Edilson Freire
Universidade Federal Rural do Rio de Janeiro, Instituto de Ciências Exatas, Departamento de Química, Rodovia BR 465, Km 7, CEP 23.890-000 Seropédica, RJ, Brazil.
Bioorg Med Chem. 2008 Mar 15;16(6):2984-91. doi: 10.1016/j.bmc.2007.12.049. Epub 2007 Dec 25.
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.
我们在此描述了九种源自天然胡椒碱的新型1,3,4 - 噻二唑鎓 - 2 - 苯胺氯化物的合成与表征。我们评估了它们对克氏锥虫不同进化形式以及宿主细胞（小鼠巨噬细胞）的毒性作用。所得结果表明，中离子型盐酸盐MI具有最佳的活性谱。化合物MI可能是用于开发高效新型化疗药物的原型，可用于治疗恰加斯病。
