Metallo-β-lactamase inhibitory activity of phthalic acid derivatives
Metallo-β-lactamase inhibitory activity of phthalic acid derivatives
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DOI：
10.1016/j.bmcl.2009.07.018
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发表时间：
2009-09-01
影响因子：
2.7
通讯作者：
Kudo, Toshiaki
中科院分区：
文献类型：
--
作者：
Hiraiwa, Yukiko;Morinaka, Akihiro;Kudo, Toshiaki
4-丁基-3-甲基邻苯二甲酸被认为是金属β-内酰胺酶抑制剂。取代邻苯二甲酸类化合物的构效关系研究表明，3-苯基邻苯二甲酸类化合物具有很强的IMP-1抑制活性。另一方面，3-取代的4-羟基苯基邻苯二甲酸衍生物与比阿培南（BIPM）对产生IMP-1的铜绿假单胞菌显示出有效的联合作用。(C)2009爱思唯尔有限公司版权所有。
4-Butyl-3-methylphthalic acid was recognized as a metallo-beta-lactamase inhibitor. The structure-activity relationship study of substituted phthalic acids afforded 3-phenylphthalic acid derivatives as potent IMP-1 inhibitors. On the other hand, 3-substituted with 4-hydroxyphenyl phthalic acid derivative displayed a potent combination effect with biapenem (BIPM) against Pseudomonas aeruginosa that produce IMP-1. (C) 2009 Elsevier Ltd. All rights reserved.