RESUMO
A number of semisynthetic rifamycin derivatives modified at position 3 and/or 4, belonging to general structures 2 and 4 (see Scheme 1), have been obtained. The synthesis and the biological activities of the new compounds are described. Compounds 4p and 4q display very good antimycobacterial activity in mice.
Assuntos
Rifamicinas/síntese química , Animais , Bactérias/efeitos dos fármacos , Feminino , Indicadores e Reagentes , Espectroscopia de Ressonância Magnética , Camundongos , Testes de Sensibilidade Microbiana , Mycobacterium tuberculosis/efeitos dos fármacos , Rifampina/toxicidade , Rifamicinas/toxicidade , Relação Estrutura-AtividadeRESUMO
A number of semisynthetic rifamycin derivatives, modified at position 3, belonging to general structures (II), (III), (IV), (V), (VI), (VII) and (VIII) (see Scheme), have been prepared. The synthesis, structure, and antimicrobial evaluation of the new compounds are described. All the derivatives have in vitro antibacterial activities comparable with that of rifampicin.
Assuntos
Bactérias/efeitos dos fármacos , Rifamicinas/síntese química , Fenômenos Químicos , Química , Espectroscopia de Ressonância Magnética , Testes de Sensibilidade Microbiana , Mycobacterium tuberculosis/efeitos dos fármacos , Rifamicinas/farmacologiaRESUMO
A number of semisynthetic rifamycin derivatives modified at positions 3 and/or 4, belonging to general structures 3, 5, and 6 (see Scheme 1), have been prepared. The synthesis, structure and antimicrobial evaluation of the new compounds are described. All the derivatives have "in vitro" antibacterial activities well comparable with that of rifampicin.