| Literature DB >> 24433862 |
Timothy A Blizzard1, Helen Chen2, Seongkon Kim2, Jane Wu2, Rena Bodner2, Candido Gude2, Jason Imbriglio2, Katherine Young3, Young-Whan Park3, Aimie Ogawa3, Susan Raghoobar3, Nichelle Hairston3, Ronald E Painter3, Doug Wisniewski3, Giovanna Scapin2, Paula Fitzgerald2, Nandini Sharma2, Jun Lu2, Sookhee Ha2, Jeff Hermes3, Milton L Hammond4.
Abstract
β-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 β-lactamase mediated antibiotic resistance. The piperidine analog 3 (MK-7655) inhibited both class A and C β-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® is currently in phase II clinical trials for the treatment of Gram-negative bacterial infections.Entities:
Keywords: Antibacterial; Antibiotic; Imipenem; MK-7655; β-Lactamase inhibitor
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Year: 2014 PMID： 24433862 DOI： 10.1016/j.bmcl.2013.12.101
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823