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    • 10. 发明授权
    • Method of using reduction products of everninomicins as antibacterial
agents and pharmaceutical compositions useful therefor
    • 使用everninomicins的还原产物作为抗菌剂的方法和用于其的药物组合物
    • US4006225A
    • 1977-02-01
    • US570117
    • 1975-04-21
    • Ashit K. GangulyOlga Sarre
    • Ashit K. GangulyOlga Sarre
    • C07H19/01A61K31/70
    • C07H19/01
    • Everninomicin antibiotics having a nitro function, e.g. everninomicin B, everninomicin C, and everninomicin D, upon treatment with aluminum amalgam in aqueous alkanol are converted to a mixture of at least two reduction products having antibacterial activity, said reduction products being an everninomicin having a nitroso function and an everninomicin having a hydroxylamino function. The nitrosoeverninomicins are also prepared by treating the corresponding hydroxylaminoeverninomicin with an oxidizing reagent selected from the group consisting of aerial oxidation in alkaline solution, and an alkali metal hypobromite in an aprotic solvent. The everninomicin reduction products and salts thereof are described as well as nitrone derivatives of the hydroxylaminoeverninomicins and salts thereof, all of which possess antibacterial activity. A preferred compound is hydroxylaminoeverninomicin D, particularly the sodium salt thereof.
    • 具有硝基功能的Everninomicin抗生素,例如 everninomicin B,everninomicin C和everninomicin D在铝链烷醇水溶液处理后,转化为具有抗菌活性的至少两种还原产物的混合物,所述还原产物是具有亚硝基功能的乙酰氨基葡蛋白酶和具有羟基氨基官能团的依托米酮 。 还可以通过用选自碱性溶液中的空气氧化的氧化剂和非质子溶剂中的碱金属次溴酸盐处理相应的羟基氨基炔诺酮来制备亚硝基诺霉素。 还描述了依维生素A还原产物及其盐以及羟基氨基炔诺酮及其盐的硝酮衍生物,它们都具有抗菌活性。 优选的化合物是D-氨基甘氨酸,尤其是其钠盐。