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.