邻苯二甲酸衍生物的金属β-内酰胺酶抑制活性
Metallo-beta-lactamase inhibitory activity of phthalic acid derivatives.
作者信息
Hiraiwa Yukiko, Morinaka Akihiro, Fukushima Takayoshi, Kudo Toshiaki
机构信息
Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd., 760 Morooka-cho, Kohoku-ku, Yokohama, Japan.
出版信息
Bioorg Med Chem Lett. 2009 Sep 1;19(17):5162-5. doi: 10.1016/j.bmcl.2009.07.018. Epub 2009 Jul 9.
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.
4-丁基-3-甲基邻苯二甲酸被认为是一种金属β-内酰胺酶抑制剂。对取代邻苯二甲酸的构效关系研究得到了3-苯基邻苯二甲酸衍生物作为有效的IMP-1抑制剂。另一方面，用4-羟基苯基取代的3-邻苯二甲酸衍生物与比阿培南（BIPM）联合使用时，对产生IMP-1的铜绿假单胞菌显示出强大的抗菌效果。
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