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ID: ALA1143438

Journal: Bioorg Med Chem Lett

Title: N-Glycine-sulfonamides as potent dual orexin 1/orexin 2 receptor antagonists.

Authors: Aissaoui H, Koberstein R, Zumbrunn C, Gatfield J, Brisbare-Roch C, Jenck F, Treiber A, Boss C.

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.

CiteXplore: 18845436

DOI: 10.1016/j.bmcl.2008.09.079