Design, synthesis, and pharmacological effects of structurally simple ligands for MT 1 and MT 2 melatonin receptors

…, V Lucini, M Pannacci, F Scaglione, C Franchini

Index: Carocci, Alessia; Catalano, Alessia; Lovece, Angelo; Lentini, Giovanni; Duranti, Andrea; Lucini, Valeria; Pannacci, Marilou; Scaglione, Francesco; Franchini, Carlo Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 17 p. 6496 - 6511

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Citation Number: 30

Abstract

A series of phenoxyalkyl and phenylthioalkyl amides were prepared as melatoninergic ligands. Modulation of affinity of the newly synthesized compound by applying SARs around the terminal amide moiety, the alkyl chain, and the methoxy group on the aromatic ring provides compounds with nanomolar affinity for both melatonin receptor subtypes. Affinity towards MT1 and MT2 receptors were modulated also exploiting chirality. The ...