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

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

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.

[1] T. Oki,et al. New antifungal antibiotics pradimicins FA-1 and FA-2: D-serine analogs of pradimicins A and C. , 1990, The Journal of antibiotics.

[2] T. Oki,et al. New antifungal antibiotics, pradimicins D and E. Glycine analogs of pradimicins A and C. , 1990, The Journal of antibiotics.

[3] T. Oki,et al. Pradimicins A, B and C: new antifungal antibiotics. I. Taxonomy, production, isolation and physico-chemical properties. , 1990, The Journal of antibiotics.

[4] T. Oki,et al. Pradimicins A, B and C: new antifungal antibiotics. II. In vitro and in vivo biological activities. , 1990, The Journal of antibiotics.

[5] T. Oki,et al. Biosynthesis of pradimicin A , 1989 .

[6] H. Kawaguchi,et al. The structure of pradimicins A, B and C: a novel family of antifungal antibiotics , 1989 .

[7] H. Kawaguchi,et al. Pradimicin, a novel class of potent antifungal antibiotics. , 1988, The Journal of antibiotics.

[8] H. Naganawa,et al. The structures of new antifungal antibiotics, benanomicins A and B. , 1988, The Journal of antibiotics.

[9] H. Naganawa,et al. New antifungal antibiotics, benanomicins A and B from an actinomycete. , 1988, The Journal of antibiotics.

[10] F. Wilcoxon,et al. A simplified method of evaluating dose-effect experiments. , 1948, The Journal of pharmacology and experimental therapeutics.