Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594640 | Bioorganic & Medicinal Chemistry Letters | 2012 | 7 Pages |
Abstract
Recent findings showing a relation between mutations in the NaV1.7 channel in humans and altered pain sensation has contributed to increase the attractiveness of this ion channel as target for development of potential analgesics. Amido chromanes 1 and 2 were identified as blockers of the NaV1.7 channel and analogues with modifications of the 5-substituent and the carboxamide part of the molecule were prepared to establish the structure-activity relationship. Compounds 13 and 29 with good overall in vitro and in vivo rat PK profile were identified. Furthermore, 29 showed in vivo efficacy in a nociceptive pain model.
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Inger Kers, Gabor Csjernyik, Istvan Macsari, Martin Nylöf, Lars Sandberg, Karin Skogholm, Tjerk Bueters, Anders B. Eriksson, Sandra Oerther, Per-Eric Lund, Elisabet Venyike, Jan-Erik Nyström, Yevgeni Besidski,