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

…, A Ogawa, S Raghoobar, RE Painter, N Hairston…

Index: 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. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 3 p. 918 - 921

Full Text: HTML

Citation Number: 19

Abstract

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