期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 21, 页码 5729-5733出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.09.079
关键词
Orexin; Dual orexin antagonist; N-Glycine-sulfonamide; Oral bioavailability; Brain penetration
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. (C) 2008 Elsevier Ltd. All rights reserved.
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