申请人:Rhone-Poulenc Sante
公开号:US04668669A1
公开(公告)日:1987-05-26
Pristinamycin II.sub.B derivatives of formula: ##STR1## in which R denotes a nitrogen-containing 4 to 7-membered heterocyclic ring optionally substituted by alkyl; or alkyl (2 to 4 C) substituted by 1 or 2 phenyl, cycloalkylamino or N-alkyl-N-cycloalkylamino (3 to 6 ring atoms), alkylamino, dialkylamino or dialkylcarbamoyloxy radicals (the dialkylamino moieties of these 2 latter radicals being capable of forming a 4 to 7-membered cyclic ring optionally substituted by alkyl) or substituted by 1 or 2 nitrogen-containing 4 to 7 membered heterocyclic rings, optionally substituted by alkyl, at least one of the above substituents being a nitrogen-containing substituent capable of forming salts and n is 1 or 2, all the alkyls being linear or branched and containing (unless stated otherwise) 1 to 10 carbon atoms, their isomers, their salts and their preparation. These compounds, optionally in combination with known synergistins or synergistins of formula: ##STR2## are useful as antimicrobial agents.
Pristinamycin II.sub.B的衍生物的化学式如下:##STR1##其中R代表一个含氮的4至7元杂环,该环可以选择性地被烷基取代;或者是烷基(2至4个碳原子)被1或2个苯基、环烷基氨基或N-烷基-N-环烷基氨基(3至6个环原子)、烷基氨基、二烷基氨基或二烷基氨基羰氧基取代(后两者的二烷基氨基团可以形成一个4至7元杂环,可以选择性地被烷基取代),或者是被1或2个含氮的4至7元杂环取代,这些环可以选择性地被烷基取代,上述取代基中至少有一个是能形成盐的含氮取代基,n为1或2,所有烷基都是直链或支链烷基,含有1至10个碳原子,它们的异构体、盐和制备方法。这些化合物与已知的协同素或化学式为:##STR2##的协同素结合使用作为抗微生物剂。