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    • 2. 发明公开
    • PENEM DERIVATIVES AND ANTIMICROBIAL AGENT CONTAINING THE SAME
    • 印度尼西亚反犹太人解放阵线
    • EP0757051A1
    • 1997-02-05
    • EP96902477.7
    • 1996-02-19
    • SUNTORY LIMITED
    • ISHIGURO, MasajiNAKATSUKA, TakashiTANAKA, RieNAMIKAWA, KoshiMATSUKI, Shinsuke
    • C07D499/88A61K31/43
    • C07D499/88Y02P20/55
    • A penem derivative represented by the following formula (I):
      wherein R 1 represents a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted alkylthio group, a substituted or unsubstituted alkenylthio group, a substituted or unsubstituted aralkylthio group, a substituted or unsubstituted arylthio group, a substituted or unsubstituted heterocyclic group, a substituted or unsubstituted heterocyclic thio group, a substituted or unsubstituted acylthio group, a mercapto group or a hydrogen atom, and R 2 represents a hydrogen atom or a carboxyl-protecting group; or a pharmacologically acceptable salt thereof.
      The compound (I) exhibits strong antibacterial activities, and especially, shows strong activities against MRSA. It is therefore useful not only as a general antibacterial agent but also as an antibacterial agent for MRSA against which no general antibacterial agents are recognized to be effective.
    • 由下式(I)表示的pen嗪衍生物:其中R 1表示取代或未取代的烷基,取代或未取代的烯基,取代或未取代的芳烷基,取代或未取代的芳基,取代或未取代的芳基 取代或未取代的芳硫基,取代或未取代的芳硫基,取代或未取代的杂环基,取代或未取代的杂环硫基,取代或未取代的酰硫基,巯基或巯基 氢原子,R 2表示氢原子或羧基保护基; 或其药理学上可接受的盐。 化合物(I)表现出强烈的抗菌活性,特别是对MRSA具有强烈的活性。 因此,不仅可以作为普通抗菌剂,而且作为MRSA的抗菌剂也是有用的,因为没有一般的抗菌剂被认为是有效的。