N-(substituted-anilinoethyl) amides: design, synthesis, and pharmacological characterization of a new class of melatonin receptor ligands

…, M Pannacci, F Fraschini, F Scaglione…

Index: Rivara, Silvia; Lodola, Alessio; Mor, Marco; Bedini, Annalida; Spadoni, Gilberto; Lucini, Valeria; Pannacci, Marilou; Fraschini, Franco; Scaglione, Francesco; Sanchez, Rafael Ochoa; Gobbi, Gabriella; Tarzia, Giorgio Journal of Medicinal Chemistry, 2007 , vol. 50, # 26 p. 6618 - 6626

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Citation Number: 61

Abstract

A novel series of melatonin receptor ligands, characterized by a N-(substituted-anilinoethyl) amido scaffold, along with preliminary structure–activity relationships (SARs), is presented. MT1 and MT2 receptor binding affinity and intrinsic activity have been modulated by the introduction of different substituents on the aniline nitrogen, on the benzene ring, and on the amide side chain. Modulation of intrinsic activity and MT2 selectivity of the newly ...