| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1372918 | Bioorganic & Medicinal Chemistry Letters | 2011 | 6 Pages |
Abstract
Blocking of certain sodium channels is considered to be an attractive mechanism to treat chronic pain conditions. Phenyl isoxazole carbamate 1 was identified as a potent and selective NaV1.7 blocker. Structural analogues of 1, both carbamates, ureas and amides, were proven to be useful in establishing the structure–activity relationship and improving ADME related properties. Amide 24 showed a good overall in vitro profile, that translated well to rat in vivo PK.
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Authors
Istvan Macsari, Lars Sandberg, Yevgeni Besidski, Ylva Gravenfors, Tobias Ginman, Johan Bylund, Tjerk Bueters, Anders B. Eriksson, Per-Eric Lund, Elisabet Venyike, Per I. Arvidsson,