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J Antibiot (Tokyo) ; 29(9): 907-14, 1976 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-1033178

RESUMO

Erythromycin A cyclic 11,12-carbonate, a compound with high antibacterial activity, forms with L-aspartic acid a salt possessing valuable properties as a potential chemotherapeutic agent. The L-aspartate of erythromycin A cyclic 11,12-carbonate exhibits strong anti-bacterial activity, especially against Gram-positive bacteria and shows low toxicity. The serum and the lung tissue levels of the discussed salt after a single dose administration to a rat were measured in comparison with those of erythromycin, its L-aspartate, erythromycin cyclic 11,12-carbonate and its L-glutamate. The new erythromycin derivative showed definitely superior characteristics to those of the other substances tested. The activity of the L-aspartate of erythromycin A cyclic 11,12-carbonate in chemotherapy of experimental staphylococcal infection and experimental pneumococcal bronchopneumonia in mice is superior to that of the parent carbonate and erythromycin itself.


Assuntos
Eritromicina/análogos & derivados , Animais , Bactérias/efeitos dos fármacos , Fenômenos Químicos , Química , Eritromicina/metabolismo , Eritromicina/farmacologia , Feminino , Absorção Intestinal , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Ratos , Infecções Estafilocócicas/tratamento farmacológico , Infecções Estreptocócicas/tratamento farmacológico , Fatores de Tempo
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