OP0595, a new diazabicyclooctane: mode of action as a serine [Beta]-lactamase inhibitor, antibiotic and [Beta]-lactam 'enhancer'

The production of a growing diversity of β-lactamases by Gram-negative bacteria challenges antimicrobial chemotherapy. OP0595, discovered separately by each of Meiji Seika Pharma and Fedora Pharmaceuticals, is a new diazabicyclooctane serine β-lactamase inhibitor that also acts as an antibiotic and...

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Bibliographic Details
Published in:Journal of antimicrobial chemotherapy 2015-10, Vol.70 (10), p.2779
Main Authors: Morinaka, Akihiro, Tsutsumi, Yuko, Yamada, Mototsugu, Suzuki, Kenji, Watanabe, Takashi, Abe, Takao, Furuuchi, Takeshi, Inamura, Seiichi, Sakamaki, Yoshiaki, Mitsuhashi, Nakako, Ida, Takashi, Livermore, David M
Format: Article
Language:English
Subjects:
Antibiotics
Chemotherapy
Gram-negative bacteria
Microbiology
Morphology
Online Access:Get full text
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Summary:The production of a growing diversity of β-lactamases by Gram-negative bacteria challenges antimicrobial chemotherapy. OP0595, discovered separately by each of Meiji Seika Pharma and Fedora Pharmaceuticals, is a new diazabicyclooctane serine β-lactamase inhibitor that also acts as an antibiotic and as a β-lactamase-independent β-lactam 'enhancer'. Inhibitory activity against serine β-lactamases and affinity for PBPs were determined using nitrocefin and Bocillin FL, respectively. MICs alone and in combination with β-lactam agents were measured according to CLSI recommendations. Morphological changes in Escherichia coli were examined by phase-contrast microscopy. IC...s of OP0595 for class A and C β-lactamases were
ISSN:0305-7453
1460-2091