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

Timothy A Blizzard,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

Bioorganic & Medicinal Chemistry Letters（2009）

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摘要
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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