2-Aminopropane-1,2,3-tricarboxylic acid:: Synthesis and co-crystallization with the class A β-lactamase BS3 of Bacillus licheniformis
2-Aminopropane-1,2,3-tricarboxylic acid:: Synthesis and co-crystallization with the class A β-lactamase BS3 of Bacillus licheniformis
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DOI：
10.1016/j.bmcl.2008.05.045
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发表时间：
2008-07-01
影响因子：
2.7
通讯作者：
Marchand-Brynaert, Jacqueline
中科院分区：
文献类型：
--
作者：
Beck, Josephine;Sauvage, Eric;Marchand-Brynaert, Jacqueline
标题化合物 4 由甘氨酸乙酯分四步制备而成，总产率为 63%。这种柠檬酸的氨基类似物已与地衣芽孢杆菌的 A 类 β-内酰胺酶 BS3 共结晶，并通过 X 射线衍射充分分析了复合物的结构。氨基柠檬酸三乙酯 3 和游离三酸 4 已针对来自所有不同亚组的成员 β-内酰胺酶进行了测试。它们是新型 A 类 β-内酰胺酶抑制剂，其作用仍然温和，但比柠檬酸盐和异柠檬酸盐更有效。 (C) 2008 Elsevier Ltd. 保留所有权利。
The title compound 4 has been prepared in four steps from ethylglycinate in 63% overall yield. This amino analog of citric acid has been co-crystallized with the class A beta-lactamase BS3 of Bacillus licheniformis and the structure of the complex fully analyzed by X-ray diffraction. Tris-ethyl aminocitrate 3 and the free tris-acid 4 have been tested against a member b- lactamase from all distinct subgroups. They are novel inhibitors of class A beta-lactamases, still modest but more potent than citrate and isocitrate. (C) 2008 Elsevier Ltd. All rights reserved.