Reactions of the polyene macrolide antibiotic nystatin with trialkylchlorosilanes led to the formation of N-alkylsilyl derivatives. The physicochemical and biological properties of the resulting nystatin derivatives were studied. Organic silicon derivatives of nystatin had high levels of antifungal activity against a wide set of test strains. Biological studies showed that the acute toxicity (LD 50 ) of the resulting nystatin derivatives were 2 -3 times lower than that of the initial antibiotic. 322 0091-150X/08/4206-0322
N-Benzyl derivatives of the polyene macrolide antibiotic amphotericin B were formed by reacting it with benzaldehydes and cyanoborohydride under reductive amination conditions. The physicochemical and biological properties of the resulting amphotericin B derivatives were studied. The N-benzyl derivatives of amphotericin B had high antifungal activity against a broad range of test cultures. Biological studies found that the acute toxicity of the amphotericin B derivatives was three times less than for the starting antibiotic.
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