2. Academic Validation
  3. Oxadiazolone bioisosteres of pregabalin and gabapentin

Oxadiazolone bioisosteres of pregabalin and gabapentin

  • Bioorg Med Chem Lett. 2009 Jan 1;19(1):247-50. doi: 10.1016/j.bmcl.2008.10.101.
David J Wustrow 1,  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,  Andrew J Thorpe,  Jacob B Schwarz
Affiliations

Affiliation

  • 1 Pfizer Global Research and Development, Groton, CT 06340, USA.
PMID: 19010672 DOI: 10.1016/j.bmcl.2008.10.101
Abstract

A series of oxadiazolone bioisosteres of pregabalin 1 and gabapentin 2 were prepared, and several were found to exhibit similar potency for the alpha(2)-delta 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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