Synthesis of quinoline derivatives as 5-HT4 receptor ligands

A Hanna-Elias, DT Manallack, I Berque-Bestel…

Index: Hanna-Elias, Amir; Manallack, David T.; Berque-Bestel, Isabelle; Irving, Helen R.; Coupar, Ian M.; Iskander, Magdy N. Australian Journal of Chemistry, 2009 , vol. 62, # 2 p. 150 - 156

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Citation Number: 5

Abstract

Abstract A general and convenient synthesis of 6-methoxyquinoline-3-carboxamides commencing with a cyclization step that involves ρ-anisidine and diethyl (ethoxymethylene) malonate is described. An additional tetrahydroquinoline scaffold 19 is prepared from 6- methoxyquinoline-3-carboxamide and this represents a novel serotinergic lead structure. These compounds show reasonable affinity at 1× 10–6 M, and docking experiments ...