| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10596843 | Bioorganic & Medicinal Chemistry Letters | 2010 | 6 Pages |
Abstract
Optimization of the novel alpha-2-delta-1 ligand 4 provided compounds 37 and 38 which have improved DMPK profiles, good in vivo analgesic activity and in vitro selectivity over alpha-2-delta-2. An in-house P-gp prediction programme and the MetaSite® software package were used to help solve the specific problems of high P-gp efflux and high in vivo clearance.
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
James W. Myatt, Mark P. Healy, Gianpaolo S. Bravi, Andrew Billinton, Christopher N. Johnson, Kim L. Matthews, Karamjit S. Jandu, Wenjing Meng, Anne Hersey, David G. Livermore, Clement B. Douault, Jason Witherington, Rino A. Bit, James E. Rowedder,