Microwave-Assisted Synthesis, Antiparasitic Activity and QSAR Studies of Substituted Quinolines

G. C. MUSCIA, M. BOLLINI, A. BRUNO, S. ASÍS

San Pedro

Simposio; 3rd. Brazilian Symposium on Medicinal Chemistry; 2006

Sociedade Brasileira de Química

Parasitic infections such as leishmaniasis, trypanosomiasis and malaria have significant impacts in third world countries and are the major reasons of mortality. Conventional therapies are often inadequate, toxic or are becoming less effective due to the emergence of numerous resistances. We have reported recently a series of 3-aminoquinolin-2-one derivatives that exhibited weak to moderate activity against P. falciparum. In order to improve these results we have synthesized in good yields two series of quinoline derivatives Friedländer and Döbner reactions employing microwave irradiation. These compounds were tested in vitro against the parasites causative of malaria, leishmania, sleeping sickness and Chagas´disease. Several derivatives showed activity against both P. falciparum and while one compound was selected for further in vivo screening. Other group of quinolines demonstrated selectivity against L. infantum. QSAR studies were carried out taking into account different physicochemical parameters and some correlations were found.