| 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 |
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| 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. |
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| 作者姓名： | 尹述凡 毛文仁 |
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| 作者单位： | 华西医科大学药学院,成都610041 |
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| 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。
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| 关 键 词： | 单环β-内酰胺 β-内酰胺酶抑制剂 4-(3-酰氨基-2-氧-吖丁啶基-1)-环己甲酸 4-(3-酰氨基-2-氧-吖丁啶基-1)苯甲酸 2-氧-吖丁啶 |
| 收稿时间： | 1989-01-26 |
Synthesis and inhibition on beta-lactamase of 4-(3-amido-4-substituted phenyl-2-oxo-azetidinonyl-1)methyl-cyclohexane carboxylic acids and -benzoic acids |
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| SF Yin and WR Mao.Synthesis and inhibition on beta-lactamase of 4-(3-amido-4-substituted phenyl-2-oxo-azetidinonyl-1)methyl-cyclohexane carboxylic acids and -benzoic acids[J].Acta Pharmaceutica Sinica,1990,25(5):340-344. |
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| Authors: | SF Yin and WR Mao |
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| Institution: | School of Pharmacy, West China University of Medical Sciences, Chengdu. |
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| Abstract: | Eleven title compounds have been synthesized from trans-4-amino-methyl-cyclohexylic acid and 4-aminomethyl-benzoic acid, and were identified via elemental analysis, IR, 1HMNR and MS. Their beta-lactamase inhibition activity was determined and contrasted with penicillanic acid S-dioxide. The results of the preliminary test show that all the products have beta-lactamase inhibition activity to some extent. |
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| Keywords: | β-Lactamase inhibitor 4-(3-Amido-2-oxo-azetidinonyl-1) cyclohexane carboxylic acid 4-(3-A-mido-2-oxo-azetidinonyl-1)-benzoic acid 2-Oxo-azetidine Monocyclic β-lactam |
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