作为高效MT(2)选择性褪黑素配体的取代N-[3-(3-甲氧基苯基)丙基]酰胺的合成
Synthesis of substituted N-[3-(3-methoxyphenyl)propyl] amides as highly potent MT(2)-selective melatonin ligands.
作者信息
Hu Yueqing, Ho Maurice K C, Chan King H, New David C, Wong Yung H
机构信息
Department of Biochemistry, the Biotechnology Research Institute, and the Molecular Neuroscience Centre, Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong.
出版信息
Bioorg Med Chem Lett. 2010 Apr 15;20(8):2582-5. doi: 10.1016/j.bmcl.2010.02.084. Epub 2010 Feb 25.
A series of substituted N-[3-(3-methoxyphenyl)propyl] amides were synthesized and their binding affinities towards human melatonin MT(1) and MT(2) receptors were evaluated. It was discovered that a benzyloxyl substituent incorporated at C6 position of the 3-methoxyphenyl ring dramatically enhanced the MT(2) binding affinity and at the same time decreased MT(1) binding affinity.
合成了一系列取代的N-[3-(3-甲氧基苯基)丙基]酰胺，并评估了它们对人褪黑素MT(1)和MT(2)受体的结合亲和力。发现3-甲氧基苯环C6位引入苄氧基取代基可显著增强MT(2)结合亲和力，同时降低MT(1)结合亲和力。
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