Title of article
Synthesis and structure–activity relationship of 1H-indole-3-carboxylic acid pyridine-3-ylamides: A novel series of 5-HT2C receptor antagonists
Author/Authors
Chul Min Park، نويسنده , , So Young Kim، نويسنده , , Woo-Kyu Park، نويسنده , , No Sang Park، نويسنده , , Churl-Min Seong، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
4
From page
3844
To page
3847
Abstract
A novel series of 1H-indole-3-carboxylic acid pyridine-3-ylamides were synthesized and identified to show high affinity and selectivity for 5-HT2C receptor. Among them, 1H-indole-3-carboxylic acid[6-(2-chloro-pyridin-3-yloxy)-pyridin-3-yl]-amide (15k) exhibits the highest affinity (IC50 = 0.5 nM) with an excellent selectivity (>2000 times) over other serotonin (5-HT1A, 5-HT2A, and 5-HT6) and dopamine (D2–D4) receptors.
Keywords
Anxiety , 5-HT2C receptor antagonists , depression , GPCR
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799665
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