Title of article
N-Acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: The first orexin-2 receptor selective non-peptidic antagonist
Author/Authors
Masaaki Hirose، نويسنده , , Shin-Ichiro Egashira، نويسنده , , Yasuhiro Goto، نويسنده , , Takashi Hashihayata، نويسنده , , Norikazu Ohtake، نويسنده , , Hisashi Iwaasa، نويسنده , , Mikiko Hata، نويسنده , , Takehiro Fukami، نويسنده , , Akio Kanatani، نويسنده , , Koji Yamada، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2003
Pages
3
From page
4497
To page
4499
Abstract
The identification of potent and selective orexin-2 receptor (OX2R) antagonists is described based on the modification of N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline analogue 1, recently discovered during high throughput screening (HTS). Substitution of an acyl group in 1 with tert-Leucine (tert-Leu), and introduction of a 4-pyridylmethyl substituent onto the amino function of tert-Leu improved compound potency, selectivity, and water solubility. Thus, compound 29 is a promising tool to investigate the role of orexin-2 receptors
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2003
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
793810
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