Article
Synthesis of (3,4-dimethoxyphenoxy)alkylamino acetamides as orexin-2 receptor antagonists.
Bioorganic & medicinal chemistry letters - 15 Oct 2008
Cole Andrew G, Stroke Ilana L, Qin Lan-Ying, Hussain Zahid, Simhadri Srilatha, Brescia Marc-Raleigh, Waksmunski Frank S, Strohl Barbara, Tellew John E, Williams John P, Saunders John, Appell Kenneth C, Henderson Ian, Webb Maria L
Abstract excerpt
The discovery and synthesis of a series of (dimethoxyphenoxy)alkylamino acetamides as orexin-2 receptor antagonists from a small-molecule combinatorial library using a high-throughput calcium mobilization functional assay (HEK293-human OX2-R cell line) is described. Active compounds show a good correlation between high-throughput single concentration screening data and measured IC(50)s. Specific examples exhibit...
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