Artigo
Synthesis and in vitro evaluation of potential antichagasic dipeptide prodrugs of primaquine
Fecha
1997-10-01Registro en:
Journal of Pharmaceutical Sciences. Washington: Amer Pharmaceutical Assn, v. 86, n. 10, p. 1127-1131, 1997.
0022-3549
10.1021/js970006v
WOS:A1997XZ45900010
Autor
Universidade de São Paulo (USP)
Universidade Estadual Paulista (Unesp)
Resumen
American trypanosomiasis (Chagas' disease) is an endemic parasitic disease afflicting more than 20 million people in Latin America. Currently, therapy is unsatisfactory and only two drugs are available. Primaquine, an antimalarial drug, has trypanocidal activity. Dipeptide derivatives of primaquine, Phe-Arg-PQ, Lys-Arg-PQ, and Phe-Ala-PQ, were synthesized. The choice of the peptides was based on the primary specificity of cruzipain, the major cysteine proteinase from T. cruzi. The prodrugs obtained were tested on the LLC-MK2 cell culture infected with trypomastigotes forms of T. cruzi Phe-Arg-PQ, Lys-Arg-PQ, and Phe-Ala-PQ were active in all stages.