Synthesis and Biochemical Evaluation of Selective Inhibitors of Class II Fructose Bisphosphate Aldolases: Towards New Synthetic Antibiotics
Synthesis and Biochemical Evaluation of Selective Inhibitors of Class II Fructose Bisphosphate Aldolases: Towards New Synthetic Antibiotics
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DOI：
10.1002/chem.200800857
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发表时间：
2008-01-01
影响因子：
4.3
通讯作者：
Therisod, Michel
中科院分区：
文献类型：
--
作者：
Fonvielle, Matthieu;Coincon, Mathieu;Therisod, Michel
我们报告了II类（锌依赖性）果糖二磷酸醛缩酶的选择性抑制剂的合成和生化评价。活性最高的化合物是果糖二磷酸的简化类似物，带有一个位置良好的金属螯合基团。它是分离的II类醛缩酶的强有力和高选择性竞争性抑制剂。我们报告的晶体学研究这种抑制剂结合在活性位点的幽门螺杆菌酶。该化合物还显示出抗结核分枝杆菌分离株的活性。
We report the synthesis and biochemical evaluation of selective inhibitors of class II (zinc-dependent) fructose bisphosphate aldolases. The most active compound is a simplified analogue of fructose bisphosphate, bearing a well-positioned metal chelating group. It is a powerful and highly selective competitive inhibitor of isolated class II aldolases. We report crystallographic studies of this inhibitor bound in the active site of the Helicobacter pylori enzyme. The compound also shows activity against Mycobacterium tuberculosis isolates.