36-derivatives of rifamycins and their use as antimicrobial agents
    4.
    发明授权
    36-derivatives of rifamycins and their use as antimicrobial agents 失效
    利福霉素36衍生物及其作为抗微生物剂的用途

    公开(公告)号:US5786350A

    公开(公告)日:1998-07-28

    申请号:US792035

    申请日:1997-01-31

    CPC分类号: C07D213/80

    摘要: Rifamycin antibiotic derivatives of formulae (I) and (Ia) bearing at the position 36 a substituent selected from (C.sub.1 -C.sub.8)alkyl, halo, hydroxy, (C.sub.1 -C.sub.4)acyloxy, (C.sub.1-C.sub.4)alkoxy, (C.sub.1 -C.sub.4)alkylthio, (C.sub.1 -C.sub.4)alkylamino, di(C.sub.1-C.sub.4)alkylamino and substituted 4-oxo-3-pyridinyl carbonyloxy of formula (1) obtained by reacting rifamycin with suitably substituted malonic acid. The compounds of the invention are antimicrobial agents mainly active against gram positive bacteria and fastidious gram negative bacteria showing the considerable antimicrobial activity against the rifamypicin resistant microbial strains.

    摘要翻译: PCT No.PCT / EP94 / 01428 Sec。 371日期1996年1月22日 102(e)日期1996年1月22日PCT提交1994年5月5日PCT公布。 出版物WO94 / 28002 (Ia)式(I)和(Ia)的利福霉素抗生素衍生物在位置36具有选自(C1-C8)的取代基, 烷基,卤素,羟基,(C1-C4)酰氧基,(C1-C4)烷氧基,(C1-C4)烷硫基,(C1-C4)烷基氨基,二(C1-C4)烷基氨基和取代的4-氧代-3-吡啶基 通过使利福霉素与适当取代的丙二酸反应获得的式(1)的羰基氧基。 本发明的化合物是主要对革兰氏阳性细菌有活性的抗微生物剂和对耐赖菌素抗性微生物菌株具有相当大的抗菌活性的革兰氏阴性细菌。