RESUMO
A series of seven limonene β-amino alcohol derivatives has been regioselectively synthesised in moderate to good yields. Two of these compounds were found to be significantly effective against in vitro cultures of the Leishmania (Viannia) braziliensis promastigote form in the micromolar range. The activities found for 3b and 3f were about 100-fold more potent than the standard drug, Pentamidine, in the same test, while limonene did not display any activity. This is the first report of antileishmanial activity by limonene β-amino alcohol derivatives.
Assuntos
Animais , Camundongos , Amino Álcoois/síntese química , Antiprotozoários/síntese química , Cicloexenos/química , Leishmania braziliensis/efeitos dos fármacos , Terpenos/química , Amino Álcoois/farmacologia , Amino Álcoois/toxicidade , Antiprotozoários/farmacologia , Antiprotozoários/toxicidade , Cicloexenos/farmacologia , Cicloexenos/toxicidade , Estrutura Molecular , Testes de Sensibilidade Parasitária , Relação Estrutura-Atividade , Terpenos/farmacologia , Terpenos/toxicidadeRESUMO
A series of seven limonene beta-amino alcohol derivatives has been regioselectively synthesised in moderate to good yields. Two of these compounds were found to be significantly effective against in vitro cultures of the Leishmania (Viannia) braziliensis promastigote form in the micromolar range. The activities found for 3b and 3f were about 100-fold more potent than the standard drug, Pentamidine, in the same test, while limonene did not display any activity. This is the first report of antileishmanial activity by limonene beta-amino alcohol derivatives.
