Synthesis, trypanocidal activity and molecular modeling studies of 2-alkylaminomethylquinoline derivatives

GISELA C. MUSCIA; SILVIA CAZORLA; FERNANDA FRANK; GABRIELA BOROSKY; GRACIELA BULDAIN; SILVIA ASIS; EMILIO MALCHIODI

EUROPEAN JOURNAL OF MEDICAL CHEMISTRY

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER

Lugar: Paris; Año: 2011 vol. 46 p. 3696 - 3703

0223-5234

Research and development of new drugs effective in the treatment ofTrypanosoma cruzi infections are a real need for the 16 million people infected in the Americas. In a previous work, a quinoline derivativesubstituted by a 2-piperidylmethyl moiety showed to be active against Chagas disease and wasconsidered a lead compound for further optimization. A series of ten analogous derivatives were tested against epimastigotes as a first approach. In view of their promising results, six of them were evaluated against the blood and intracellular replicative forms of the parasite in humans. Among them, compound against the blood and intracellular replicative forms of the parasite in humans.