Synthesis of substituted N-[3-(3-methoxyphenyl) propyl] amides as highly potent MT 2-selective melatonin ligands

Y Hu, MKC Ho, KH Chan, DC New, YH Wong

Index: Hu, Yueqing; Ho, Maurice K.C.; Chan, King H.; New, David C.; Wong, Yung H. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 8 p. 2582 - 2585

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Citation Number: 32

Abstract

A series of substituted N-[3-(3-methoxyphenyl) propyl] amides were synthesized and their binding affinities towards human melatonin MT1 and MT2 receptors were evaluated. It was discovered that a benzyloxyl substituent incorporated at C6 position of the 3-methoxyphenyl ring dramatically enhanced the MT2 binding affinity and at the same time decreased MT1 binding affinity.