RESUMO

A series of 4-amino-7-chloroquinoline derivatives were synthesized by the reaction of 4,7-dichloro-quinoline with the corresponding diamine and then with propargyl bromide. In addition, platinum(II) complexes were obtained by reacting some of the organic derivatives with K(2)PtCl(4). Several of the synthesized compounds displayed antituberculosis activities. Compound 3 was 47.5 times more active than amphotericin B against Leishmania chagasi (IC(50)=0.04 µg/mL). Compounds 5, 6, 7, 9, 10, 11 and 13 presented promising results against Mycobacterium tuberculosis, with MIC values ranging from 12.5 to 15.6 µg/mL, comparable to the "first and second line" drugs used to treat tuberculosis.

Assuntos

Aminoquinolinas/síntese química , Aminoquinolinas/farmacologia , Antituberculosos/síntese química , Complexos de Coordenação/síntese química , Complexos de Coordenação/farmacologia , Leishmania/efeitos dos fármacos , Platina/química , Aminoquinolinas/química , Anfotericina B/farmacologia , Antituberculosos/química , Antituberculosos/farmacologia , Complexos de Coordenação/química , Diaminas/química , Testes de Sensibilidade Microbiana/métodos , Mycobacterium tuberculosis/efeitos dos fármacos , Pargilina/análogos & derivados , Pargilina/química