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Comparative Study
. 2010 Feb 1;20(3):918-21.
doi: 10.1016/j.bmcl.2009.12.069. Epub 2009 Dec 23.

Side chain SAR of bicyclic beta-lactamase inhibitors (BLIs). 1. Discovery of a class C BLI for combination with imipinem

Timothy A Blizzard  1 , Helen Chen, Seongkon Kim, Jane Wu, Katherine Young, Young-Whan Park, Amy Ogawa, Susan Raghoobar, Ronald E Painter, Nichelle Hairston, Sang Ho Lee, Andrew Misura, Tom Felcetto, Paula Fitzgerald, Nandini Sharma, Jun Lu, Sookhee Ha, Emily Hickey, Jeff Hermes, Milton L Hammond
Affiliations
Comparative Study

Side chain SAR of bicyclic beta-lactamase inhibitors (BLIs). 1. Discovery of a class C BLI for combination with imipinem

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

Abstract

Bridged monobactam beta-lactamase inhibitors were prepared and evaluated as potential partners for combination with imipenem to overcome class C beta-lactamase mediated resistance. The (S)-azepine analog 2 was found to be effective in both in vitro and in vivo assays and was selected for preclinical development.

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