Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part I: Influence of the substitution on the basic nitrogen and the position of the amide on …

P Carato, A Graulich, N Jensen, BL Roth…

Index: Carato, Pascal; Graulich, Amaury; Jensen, Niels; Roth, Bryan L.; Liegeois, Jean-Francois Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 6 p. 1565 - 1569

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Citation Number: 5

Abstract

A series of 1-and 2-naphthamides has been prepared and tested for in vitro binding to D2L, D4. 2, and 5-HT2A receptors. Different compounds display selectivity for D4. 2 and 5-HT2A receptors versus D2L receptors. N-(1-Arylalkyl-piperidin-4-yl) carboxamides have higher affinities than the corresponding N-(4-arylalkylamino-piperidin-1-yl) carboxamide analogues. A benzyl moiety in position 1 of the piperidine in the 2-naphthamide series (2) ...