| Autor: |
Wustrow DJ; Pfizer Global Research and Development, Groton, CT 06340, USA., Belliotti TR, Capiris T, Kneen CO, Bryans JS, Field MJ, Williams D, El-Kattan A, Buchholz L, Kinsora JJ, Lotarski SM, Vartanian MG, Taylor CP, Donevan SD, Thorpe AJ, Schwarz JB |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Jan 01; Vol. 19 (1), pp. 247-50. Date of Electronic Publication: 2008 Oct 25. |
| DOI: |
10.1016/j.bmcl.2008.10.101 |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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