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Bioorg Med Chem Lett. 2009 Sep 1;19(17):5162-5. doi: 10.1016/j.bmcl.2009.07.018. Epub 2009 Jul 9.

Metallo-beta-lactamase inhibitory activity of phthalic acid derivatives.

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  • 1Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd., 760 Morooka-cho, Kohoku-ku, Yokohama, Japan.


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.

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