RESUMO
Synthesis and biological properties of amphotericin B O-methyl oxime are described. The presence of an intact hemiketal ring in the antibiotic molecule appeared to be essential for its biological activity.
Assuntos
Anfotericina B/análogos & derivados , Anfotericina B/síntese química , Anfotericina B/farmacologia , Candida albicans/efeitos dos fármacos , Humanos , Estrutura Molecular , Saccharomyces cerevisiae/efeitos dos fármacosAssuntos
Pregnanodionas/metabolismo , Adulto , Disponibilidade Biológica , Meia-Vida , Humanos , Pregnanodionas/sangueRESUMO
A series of aliphatic amides of amphotericin B have been synthesized. The structure of the derivatives which were obtained has been established by mass spectrometry. Their biological properties: inhibition of growth of Saccharomyces cerevisiae and hemolytic activity have been determined. The quantitative relationships between the activity of amides of amphotericin B against S. cerevisiae and their lipophilicity can be expressed by a parabolic function, whereas that between hemolytic activity and lipophilicity--by polynominal expression of fourth degree.
Assuntos
Anfotericina B/análogos & derivados , Antifúngicos/síntese química , Anfotericina B/síntese química , Anfotericina B/farmacologia , Antifúngicos/farmacologia , Espectrometria de Massas , Relação Estrutura-AtividadeRESUMO
A novel carbohydrate has been isolated after acidic hydrolysis of nystatin A3, candidinin and polyfungin B and its structure established as 2,6-dideoxy-L-ribohexopyranose.
Assuntos
Antifúngicos , Desoxiaçúcares/análise , Hexoses/análise , Polienos , Fenômenos Químicos , Química , Espectrometria de MassasRESUMO
The complete structure of mycoheptin, a heptaene macrolide antifungal antibiotic, has been established as I by chemical degradation methods and MS and 1H NMR analysis of the products.