SYNTHESIS AND IN-VITRO EVALUATION OF POTENTIAL ANTICHAGASIC DIPEPTIDEPRODRUGS OF PRIMAQUINE

American trypanosomiasis (Chagas' disease) is an endemic parasitic dis ease afflicting more than 20 million people in Latin America. Currentl y, therapy is unsatisfactory and only two drugs are available. Primaqu ine, an antimalarial drug, has trypanocidal activity. Dipeptide deriva tives of primaquine, Phe-Arg-PQ, Lys-Arg-PQ, and Phe-Ala-PQ, were synt hesized. The choice of the peptides was based on the primary specifici ty of cruzipain, the major cysteine proteinase from T. cruzi. The prod rugs obtained were tested on the LLC-MK2 cell culture infected with tr ypomastigotes forms of T. cruzi Phe-Arg-PQ, Lys-Arg-PQ, and Phe-Ala-PQ were active in all stages.