Discovery and Pharmacological Profile of New 1 H-Indazole-3-carboxamide and 2 H-Pyrrolo [3, 4-c] quinoline Derivatives as Selective Serotonin 4 Receptor Ligands

…, A Capezzone de Joannon, N Cazzolla…

Index: Furlotti, Guido; Alisi, Maria Alessandra; Apicella, Claudia; Capezzone De Joannon, Alessandra; Cazzolla, Nicola; Costi, Roberta; Cuzzucoli Crucitti, Giuliana; Garrone, Beatrice; Iacovo, Alberto; Magaro, Gabriele; Mangano, Giorgina; Miele, Gaetano; Ombrato, Rosella; Pescatori, Luca; Polenzani, Lorenzo; Rosi, Federica; Vitiello, Marco; Di Santo, Roberto Journal of Medicinal Chemistry, 2012 , vol. 55, # 22 p. 9446 - 9466

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Citation Number: 11

Abstract

Since the discovery of the serotonin 4 receptor (5-HT4R), a large number of receptor ligands have been studied. The safety concerns and the lack of market success of these ligands have mainly been attributed to their lack of selectivity. In this study we describe the discovery of N-[(4-piperidinyl) methyl]-1 H-indazole-3-carboxamide and 4-[(4-piperidinyl) methoxy]-2 H- pyrrolo [3, 4-c] quinoline derivatives as new 5-HT4R ligands endowed with high selectivity ...