Metallo-β-lactamase inhibitory activity of 3-alkyloxy and 3-amino phthalic acid derivatives and their combination effect with carbapenem.
3-Alkyloxy and 3-amino phthalic acid derivatives were found to have metallo-β-lactamase inhibitory activity. Among them, 3-amino phthalic acid derivatives showed both potent activity against metallo-β-lactamase, IMP-1 inhibitory activity and a strong combination effect with biapenem (BIPM), carbapenem antibiotic. In particular, the 4'-hydroxy-piperidine derivative showed strong IMP-1 inhibitory activity and a combination effect with various antibiotics.
Pharmaceutical Research Center, Meiji Seika Pharma, Co., Ltd, Kohoku-ku, Yokohama, Japan. yukiko.hiraiwa@meiji.com
Yukiko
Y
Hiraiwa
Akihiro
A
Morinaka
Takayoshi
T
Fukushima
Toshiaki
T
Kudo
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D015780:Carbapenems / Q000737:chemistry* / Q000494:pharmacology; D004791:Enzyme Inhibitors / 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 / Q000201:enzymology; D013329:Structure-Activity Relationship; D013845:Thienamycins / Q000494:pharmacology; D065093:beta-Lactamase Inhibitors; D001618:beta-Lactamases / Q000378:metabolism
D000900:Anti-Bacterial Agents; D015780:Carbapenems; D004791:Enzyme Inhibitors; D010795:Phthalic Acids; D013845:Thienamycins; D065093:beta-Lactamase Inhibitors; C032279:phthalic acid; D001618:beta-Lactamases; C065257:biapenem
Metallo-β-lactamase; Pseudomonas aeruginosa