Water-soluble pradimicin derivatives, synthesis and antifungal evaluation of N,N-dimethyl pradimicins.

T Oki, M Kakushima, M Nishio, H Kamei, M Hirano, Y Sawada, M Konishi

Bristol-Myers Research Institute, Ltd., Tokyo Research Center, Japan.

The Journal of antibiotics 1990 Oct

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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.

Citation

T Oki, M Kakushima, M Nishio, H Kamei, M Hirano, Y Sawada, M Konishi. Water-soluble pradimicin derivatives, synthesis and antifungal evaluation of N,N-dimethyl pradimicins. The Journal of antibiotics. 1990 Oct;43(10):1230-5