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
Pages
5
From page
5729
To page
5733
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
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
800096
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