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.