Bioorganic & Medicinal Chemistry Letters 2009-09-01

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

Yukiko Hiraiwa, Akihiro Morinaka, Takayoshi Fukushima, Toshiaki Kudo

Index: Bioorg. Med. Chem. Lett. 19 , 5162-5, (2009)

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Abstract

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.