4-Substituted anilides as selective melatonin MT 2 receptor agonists

JR Epperson, JA Deskus, AJ Gentile, LG Iben…

Index: Epperson, James R.; Deskus, Jeffrey A.; Gentile, Anthony J.; Iben, Lawrence G.; Ryan, Elaine; Sarbin, Nathan S. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 4 p. 1023 - 1026

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Citation Number: 13

Abstract

A series of 4-substituted anilides with human melatonergic affinity is reported. Butyramides 26, 39, 42, 52, 57, and 58 all demonstrated subnanomolar MT2 binding affinity and MT2 selectivity of at least 70-fold over the MT1 receptor. Compound 26 demonstrated full agonism at the MT2 receptor.