Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2014 Feb 1;24(3):780-5.
doi: 10.1016/j.bmcl.2013.12.101. Epub 2014 Jan 3.

Discovery of MK-7655, a β-lactamase inhibitor for combination with Primaxin®

Timothy A Blizzard  1 , Helen Chen  2 , Seongkon Kim  2 , Jane Wu  2 , Rena Bodner  2 , Candido Gude  2 , Jason Imbriglio  2 , Katherine Young  3 , Young-Whan Park  3 , Aimie Ogawa  3 , Susan Raghoobar  3 , Nichelle Hairston  3 , Ronald E Painter  3 , Doug Wisniewski  3 , Giovanna Scapin  2 , Paula Fitzgerald  2 , Nandini Sharma  2 , Jun Lu  2 , Sookhee Ha  2 , Jeff Hermes  3 , Milton L Hammond  4
Affiliations

Discovery of MK-7655, a β-lactamase inhibitor for combination with Primaxin®

Timothy A Blizzard et al. Bioorg Med Chem Lett. .

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.

Keywords: Antibacterial; Antibiotic; Imipenem; MK-7655; β-Lactamase inhibitor.

PubMed Disclaimer

MeSH terms

LinkOut - more resources