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

Bridged monobactam b-lactamase inhibitors were prepared and evaluated as potential partners for combination with imipenem to overcome class C b-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 devel...

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Published inBioorganic & medicinal chemistry letters Vol. 20; no. 3; pp. 918 - 921
Main Authors Blizzard, Timothy A, Chen, Helen, Kim, Seongkon, Wu, Jane, Young, Katherine, Park, Young-Whan, Ogawa, Amy, Raghoobar, Susan, Painter, Ronald E, Hairston, Nichelle, Lee, Sang Ho, Misura, Andrew, Felcetto, Tom, Fitzgerald, Paula, Sharma, Nandini, Lu, Jun, Ha, Sookhee, Hickey, Emily, Hermes, Jeff, Hammond, Milton L
Format Journal Article
LanguageEnglish
Published 01.02.2010
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Summary:Bridged monobactam b-lactamase inhibitors were prepared and evaluated as potential partners for combination with imipenem to overcome class C b-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.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
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ObjectType-Feature-2
ISSN:0960-894X
DOI:10.1016/j.bmcl.2009.12.069