Synthesis and structure–activity relationship of 1H-indole-3-carboxylic acid pyridine-3-ylamides: A novel series of 5-HT2C receptor antagonists

Authors :: Park, Chul Min
Kim, So Young
Park, Woo Kyu
Park, No Sang
Seong, Churl Min
Source :: Bioorganic & Medicinal Chemistry Letters. Jul2008, Vol. 18 Issue 14, p3844-3847. 4p.
Publication Year :: 2008
Abstract: 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 =0.5nM) with an excellent selectivity (>2000 times) over other serotonin (5-HT1A, 5-HT2A, and 5-HT6) and dopamine (D2–D4) receptors. [Copyright &y& Elsevier]

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