| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10594808 | Bioorganic & Medicinal Chemistry Letters | 2014 | 6 Pages |
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.
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Authors
Timothy A. Blizzard, Helen Chen, Seongkon Kim, Jane Wu, Rena Bodner, Candido Gude, Jason Imbriglio, Katherine Young, Young-Whan Park, Aimie Ogawa, Susan Raghoobar, Nichelle Hairston, Ronald E. Painter, Doug Wisniewski, Giovanna Scapin, Paula Fitzgerald,