American Chemical Society
jm8b01389_si_001.pdf (1.62 MB)

Orally Absorbed Derivatives of the β‑Lactamase Inhibitor Avibactam. Design of Novel Prodrugs of Sulfate Containing Drugs

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journal contribution
posted on 2018-10-08, 00:00 authored by Eric M. Gordon, Matthew A. J. Duncton, Mark A. Gallop
Only one FDA-approved β-lactamase inhibitor has ever been orally available: clavulanic acid, approved in 1984. Avibactam, approved by FDA in 2015, is the first of a new class of BLIs called diazabicyclooctanes, or “DBOs”. This class has much broader coverage than clavulanic acid but can only be administered by intravenous injection. Herein, we describe the synthesis and testing of the first approved BLI to be rendered orally bioavailable since clavulanic acid (1984).