| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1375960 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Abstract
A series of oxadiazolone bioisosteres of pregabalin 1 and gabapentin 2 were prepared, and several were found to exhibit similar potency for the α2-δ subunit of voltage-gated calcium channels. Oxadiazolone 9 derived from 2 achieved low brain uptake but was nevertheless active in models of osteoarthritis. The high clearance associated with compound 9 was postulated to be a consequence of efflux by OAT and/or OCT, and was attenuated on co-administration with cimetidine or probenecid.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
David J. Wustrow, Thomas R. Belliotti, Thomas Capiris, Clare O. Kneen, Justin S. Bryans, Mark J. Field, Dic Williams, Ayman El-Kattan, Lisa Buchholz, Jack J. Kinsora, Susan M. Lotarski, Mark G. Vartanian, Charles P. Taylor, Sean D. Donevan,