RESUMO

Five (-)-cubebin derivative compounds, (-)-O-acetyl cubebin (3), (-)-O-benzyl cubebin (4), (-)-O-(N,N-dimethylaminoethyl)-cubebin (5), (-)-hinokinin (6) and (-)-6,6'-dinitrohinokinin (7), previously synthesised by our research group, were evaluated on in vitro assay against free amastigote forms of Trypanosoma cruzi, the asogic agent of Chagas' disease. It was observed that 6 was the most active compound (IC(50)=0.7 microM), and that 4 and 5 displayed moderate activity against the parasite, giving IC(50) values of 5.7 and 4.7 microM, respectively. In contrast, it was observed that compound 3 was inactive and that 7 displayed low activity with IC(50) values of congruent with 1.5 x 10(4) and 95.3 microM, respectively.

Assuntos

4-Butirolactona/análogos & derivados , Benzodioxóis/farmacologia , Lignanas/farmacologia , Glicoproteínas de Membrana/química , Proteínas de Protozoários/química , Tripanossomicidas/farmacologia , Trypanosoma cruzi/efeitos dos fármacos , 4-Butirolactona/química , 4-Butirolactona/farmacologia , 4-Butirolactona/uso terapêutico , Animais , Benzodioxóis/química , Benzodioxóis/uso terapêutico , Doença de Chagas/tratamento farmacológico , Concentração Inibidora 50 , Lignanas/química , Lignanas/uso terapêutico , Testes de Sensibilidade Parasitária , Relação Estrutura-Atividade , Tripanossomicidas/química , Tripanossomicidas/uso terapêutico