Metallo-beta-lactamase inhibitory activity of phthalic acid derivatives.
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.
Hiraiwa
Yukiko
Y
Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd., 760 Morooka-cho, Kohoku-ku, Yokohama, Japan. yukiko_hiraiwa@meiji.co.jp
Morinaka
Akihiro
A
Fukushima
Takayoshi
T
Kudo
Toshiaki
T
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D010795:Phthalic Acids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D013329:Structure-Activity Relationship; D013845:Thienamycins / Q000494:pharmacology; D065093:beta-Lactamase Inhibitors; D001618:beta-Lactamases / Q000378:metabolism
D000900:Anti-Bacterial Agents; D010795:Phthalic Acids; D013845:Thienamycins; D065093:beta-Lactamase Inhibitors; D001618:beta-Lactamases; C065257:biapenem