WATER-SOLUBLE PRADIMICIN DERIVATIVES, SYNTHESIS AND ANTIFUNGAL EVALUATION OF N, N-DIMETHYL PRADIMICINS

Abstract

Three N, N-dimethyl pradimicins were synthesized by reductive alkylation of pradimicins A, E and FA-2 and evaluated for antifungal activity, water solubility and acute toxicity in mice. They showed in vitro antifungal activity superior to pradimicin A. N, N-Dimethylpradimicins E and FA-2 showed great improvement in water solubility and animal tolerance. N, N-Dimethylpradimicin FA-2 was effective in 3 experimental in vivo fungal infection models.