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

…, J Gatfield, C Brisbare-Roch, F Jenck, A Treiber…

文献索引：Aissaoui, Hamed; Koberstein, Ralf; Zumbrunn, Cornelia; Gatfield, John; Brisbare-Roch, Catherine; Jenck, Francois; Treiber, Alexander; Boss, Christoph Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 21 p. 5729 - 5733

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被引用次数: 20

摘要

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.