Discovery of 3-aryl-3-methyl-1H-quinoline-2, 4-diones as a new class of selective 5-HT 6 receptor antagonists

CM Seong, WK Park, CM Park, JY Kong…

Index: Seong, Churl Min; Park, Woo Kyu; Park, Chul Min; Kong, Jae Yang; Park, No Sang Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 2 p. 738 - 743

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Citation Number: 26

Abstract

A 5, 7-dichloro-3-phenyl-3-methyl-quinoline-2, 4-dione (11a) has been identified in a random screen as a lead for 5-HT6 antagonist. During the lead optimization process, several analogs were synthesized and their biological activities were investigated. Within this series, several compounds display high binding affinity and selectivity for the 5-HT6 receptor. In particular, 3-(4-hydroxyphenyl)-3-methyl-quinoline-2, 4-dione (12f) exhibits high affinity (Ki ...