尹述凡, 毛文仁. 4-(3-酰氨基-4-取代苯基-2-氧-吖丁啶基-1)甲基-环己甲酸和-苯甲酸的合成及抑制β-内酰胺酶作用J. 药学学报, 1990, 25(5): 340-344.
引用本文: 尹述凡, 毛文仁. 4-(3-酰氨基-4-取代苯基-2-氧-吖丁啶基-1)甲基-环己甲酸和-苯甲酸的合成及抑制β-内酰胺酶作用J. 药学学报, 1990, 25(5): 340-344.
SF Yin, WR Mao. SYNTHESIS AND INHIBITION ON β-LACTAMASE OF 4-(3-AMIDO-4-SUBSTITUTED PHENYL-2-OXO-AZETIDINONYL-1)METHYLCYCLOHEXANE CARBOXYLIC ACIDS AND -BENZOIC ACIDSJ. Acta Pharmaceutica Sinica, 1990, 25(5): 340-344.
Citation: SF Yin, WR Mao. SYNTHESIS AND INHIBITION ON β-LACTAMASE OF 4-(3-AMIDO-4-SUBSTITUTED PHENYL-2-OXO-AZETIDINONYL-1)METHYLCYCLOHEXANE CARBOXYLIC ACIDS AND -BENZOIC ACIDSJ. Acta Pharmaceutica Sinica, 1990, 25(5): 340-344.

4-(3-酰氨基-4-取代苯基-2-氧-吖丁啶基-1)甲基-环己甲酸和-苯甲酸的合成及抑制β-内酰胺酶作用

SYNTHESIS AND INHIBITION ON β-LACTAMASE OF 4-(3-AMIDO-4-SUBSTITUTED PHENYL-2-OXO-AZETIDINONYL-1)METHYLCYCLOHEXANE CARBOXYLIC ACIDS AND -BENZOIC ACIDS

  • 摘要: 本文设计,并以反式-4-氨甲基环己基田酸和4-氨甲基苯甲酸为原料合成了11种新标题化合物,并经元素分析、红外光谱、核磁共振氢谱和质谱证实。初步抑酶活性测定表明,对腊样芽胞杆菌产生的β-内酰胺酶均有不同程度的抑制作用。

     

    Abstract: Eleven title compounds have been synthesized from trans-4-aminomethyl-cyclohexylic acid and 4-aminomethyl-benzoic acid, and were identified via elemental analysis, IR, 1HMNR and MS. Their β-lactamase inhibition activity was determined and contrasted with penicillanic acid S-dioxide. The results of the preliminary test show that all the products have β-lactamase inhibition activity to some extent.

     

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