古渠鸣, 李正化. 1-(3′,4′-二甲氧基)苯甲酰基-3-酰氨基-4-取代苯基-2-吖丁啶酮类化合物的合成及其抑制β-内酰胺酶的作用J. 药学学报, 1985, 20(12): 896-901.
引用本文: 古渠鸣, 李正化. 1-(3′,4′-二甲氧基)苯甲酰基-3-酰氨基-4-取代苯基-2-吖丁啶酮类化合物的合成及其抑制β-内酰胺酶的作用J. 药学学报, 1985, 20(12): 896-901.
Gu Qu-Ming, Li Zheng-Hua. THE SYNTHESIS OF 1- (3', 4'-DIMETHOXY) BENZOYL-3-AMIDO-4-SUBSTITUTED PHENYL-2-AZETIDINONES AND THEIR BETA-LACTAMASE INHIBITION ACTIVITIESJ. Acta Pharmaceutica Sinica, 1985, 20(12): 896-901.
Citation: Gu Qu-Ming, Li Zheng-Hua. THE SYNTHESIS OF 1- (3', 4'-DIMETHOXY) BENZOYL-3-AMIDO-4-SUBSTITUTED PHENYL-2-AZETIDINONES AND THEIR BETA-LACTAMASE INHIBITION ACTIVITIESJ. Acta Pharmaceutica Sinica, 1985, 20(12): 896-901.

1-(3′,4′-二甲氧基)苯甲酰基-3-酰氨基-4-取代苯基-2-吖丁啶酮类化合物的合成及其抑制β-内酰胺酶的作用

THE SYNTHESIS OF 1- (3', 4'-DIMETHOXY) BENZOYL-3-AMIDO-4-SUBSTITUTED PHENYL-2-AZETIDINONES AND THEIR BETA-LACTAMASE INHIBITION ACTIVITIES

  • 摘要: 本文设计和合成了14个新的1-(3′,4′-二甲氧基)苯甲酰基-3-酰氨基-4-取代苯基-2-吖丁啶酮类化合物,分别经红外光谱、核磁共振氢谱、质谱和元素分析证实。其中11个化合物具有β-内酰胺酶抑制作用。Ⅶe-1及Ⅶg-1的活性约为临床应用的青霉烷砜酸的两倍。

     

    Abstract: Fourteen novel title compounds were. designed and synthesized through cyclocondensation, deprotection, acylation and oxidative reactions. Their chemical structures were identified by elemental analysis, IR and mass spectra. The cis-configuration of these beta-lactams were determined by coupling constants in 360 MC 1HNMR spectra.The inhibition activities of these compounds to acetobacter beta-lactamase were testedprcliminarily. Eleven of them exhibited marked activities. Among them, the inhibiting activities of Ⅲe-1 and Ⅲg-1 are twice as that of sulbactam.

     

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