Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10596496 | Bioorganic & Medicinal Chemistry Letters | 2012 | 8 Pages |
Abstract
The NaV1.7 ion channel is an attractive target for development of potential analgesic drugs based on strong genetic links between mutations in the gene coding for the channel protein and inheritable pain conditions. The (S)-N-chroman-3-ylcarboxamide series, exemplified by 1, was used as a starting point for development of new channel blockers, resulting in the phenethyl nicotinamide series. The structure and activity relationship for this series was established and the metabolic issues of early analogues were addressed by appropriate substitutions. Compound 33 displayed acceptable overall in vitro properties and in vivo rat PK profile.
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Authors
Inger Kers, Istvan Macsari, Gabor Csjernyik, Martin Nylöf, Karin Skogholm, Lars Sandberg, Alexander Minidis, Tjerk Bueters, Jonas Malmborg, Anders B. Eriksson, Per-Eric Lund, Elisabet Venyike, Lei Luo, Jan-Erik Nyström, Yevgeni Besidski,