RESUMO
We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3). Hydrolysis of the methyl ester adduct (5) yielded the free acid (6). The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.
Assuntos
Aminoquinolinas/síntese química , Antiprotozoários/síntese química , Leishmania/efeitos dos fármacos , Quinolinas/química , Triptofano/análogos & derivados , Aminoquinolinas/química , Aminoquinolinas/toxicidade , Animais , Antiprotozoários/química , Antiprotozoários/toxicidade , Chlorocebus aethiops , Hidrólise , Quinolinas/síntese química , Quinolinas/toxicidade , Triptofano/síntese química , Triptofano/química , Triptofano/toxicidade , Células VeroRESUMO
This study aimed to evaluate the 4-(6'-thiopurine)-7-chloroquinoline, a novel quinoline/6-thiopurine conjugate, for the treatment of Gallus gallus experimentally infected with Plasmodium juxtanucleare, an avian malaria agent. The avian group treated with 4-(6'-thiopurine)-7-chloroquinoline showed a significative parasite clearance and maintained a low level of parasitaemia, when compared with the untreated control group and to the chloroquine treated avian group.
