Synthesis and antifungal activity of N-trialkylsilyl derivatives of nystatin

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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 (LD50) of the resulting nystatin derivatives were 2–3 times lower than that of the initial antibiotic.

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