Synthesis and structure–activity relationship of 1H-indole-3-carboxylic acid pyridine-3-ylamides: A novel series of 5-HT 2C receptor antagonists

…, SY Kim, WK Park, NS Park, CM Seong

Index: Park, Chul Min; Kim, So Young; Park, Woo Kyu; Park, No Sang; Seong, Churl Min Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 14 p. 3844 - 3847

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Citation Number: 17

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.