| Literature DB >> 18845436 |
Hamed Aissaoui1, Ralf Koberstein, Cornelia Zumbrunn, John Gatfield, Catherine Brisbare-Roch, Francois Jenck, Alexander Treiber, Christoph Boss.
Abstract
A series of dual OX(1)R/OX(2)R orexin antagonists was prepared based on a N-glycine-sulfonamide core. SAR studies of a screening hit led to compounds with low nanomolar affinity for both receptors and good oral bioavailability. One of these compounds, 47, has demonstrated in vivo activity in rats following oral administration.Entities:
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Year: 2008 PMID： 18845436 DOI： 10.1016/j.bmcl.2008.09.079
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823