期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 3, 页码 780-785出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.12.101
关键词
beta-Lactamase inhibitor; MK-7655; Antibacterial; Imipenem; Antibiotic
beta-Lactamase inhibitors with a bicyclic urea core and a variety of heterocyclic side chains were prepared and evaluated as potential partners for combination with imipenem to overcome class A and C beta-lactamase mediated antibiotic resistance. The piperidine analog 3 (MK-7655) inhibited both class A and C beta-lactamases in vitro. It effectively restored imipenem's activity against imipenem-resistant Pseudomonas and Klebsiella strains at clinically achievable concentrations. A combination of MK-7655 and Primaxin (R) is currently in phase II clinical trials for the treatment of Gram-negative bacterial infections. (C) 2014 Elsevier Ltd. All rights reserved.
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