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

2009; Elsevier BV; Volume: 20; Issue: 3 Linguagem: Inglês

10.1016/j.bmcl.2009.12.069

1464-3405

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

Antibiotics Pharmacokinetics and Efficacy

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.