Title of article :
N-Glycine-sulfonamides as potent dual orexin 1/orexin 2 receptor antagonists
Author/Authors :
Hamed Aissaoui، نويسنده , , Ralf Koberstein، نويسنده , , Cornelia Zumbrunn، نويسنده , , John Gatfield، نويسنده , , Catherine Brisbare-Roch، نويسنده , , François Jenck، نويسنده , , Alexander Treiber، نويسنده , , Christoph Boss، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2008
Abstract :
A series of dual OX1R/OX2R 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.
Keywords :
Brain penetration , Oral bioavailability , N-Glycine-sulfonamide , Orexin , Dual orexin antagonist
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters
