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    • 10. 发明授权
    • Mycoplanecin derivatives and their preparation
    • 髓鞘衍生物及其制备方法
    • US4370266A
    • 1983-01-25
    • US250709
    • 1981-04-03
    • Mamoru AraiTatsuo HaneishiMutsuo NakajimaAkio TorikataRyuzo Enokita
    • Mamoru AraiTatsuo HaneishiMutsuo NakajimaAkio TorikataRyuzo Enokita
    • A61K38/00C07K7/06C12P21/04C07C103/52
    • C12R1/045C07K7/06A61K38/00Y10S930/19Y10S930/27
    • Mycoplanecin derivatives of formula (I): ##STR1## [wherein: R represents a hydrogen atom, an N-(.alpha.-ketobutyryl)-N-methylvalyl group or an N-(.alpha.-hydroxybutyryl)-N-methylvalyl group;R.sup.1 represents a methyl group or an ethyl group; andwhen R.sup.1 represents a methyl group, R.sup.2 represents an isobutyl group and, when R.sup.1 represents an ethyl group, R.sup.2 represents a pentyl group] have antibacterial activity which is particularly pronounced against bacteria of the genus Mycobacterium. The compounds in which R represents and N-(.alpha.-ketobutyryl)-N-methylvalyl group, named Mycoplanecin B (R.sup.1 represents a methyl group) and Mycoplanecin C (R.sup.1 represents an ethyl group), may be prepared by cultivation of a microorganism of the genus Actinoplanes, while the compounds where R represents an N-(.alpha.-hydroxybutyryl)-N-methylvalyl group or a hydrogen atom can be prepared by reducing the corresponding compound where R represents an N-(.alpha.-ketobutyryl)-N-methylvalyl group or by hydrolyzing the corresponding compound where R represents an N-(.alpha.-ketobutyryl)-N-methylvalyl or N-(.alpha.-hydroxybutyryl)-N-methylvalyl group, respectively.
    • 式(I)的肌钙蛋白聚糖衍生物:其中:R表示氢原子,N-(α-酮丁酰基)-N-甲基缬氨酰基或N-(α-羟基丁酰基)-N-甲基缬氨酰基 ; R1表示甲基或乙基; 当R1表示甲基时,R2表示异丁基,当R1表示乙基时,R2表示戊基]具有对分枝杆菌属细菌特别显着的抗菌活性。 其中R表示的化合物和N-(α-酮丁酰基)-N-甲基缬氨酰基,命名为Mycoplanecin B(R1表示甲基)和Mycoplanecin C(R1表示乙基))可以通过培养 其中R代表N-(α-羟基丁酰基)-N-甲基缬氨酰基或氢原子的化合物可以通过还原相应的化合物来制备,其中R代表N-(α-酮丁酰基)-N-甲基缬氨酰基 或通过水解相应的化合物,其中R表示N-(α-酮丁酰基)-N-甲基缬氨酰基或N-(α-羟基丁酰基)-N-甲基缬氨酰基。