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

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

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

Bioorg Med Chem Lett. 2010 Apr 15;20(8):2582-5. doi: 10.1016/j.bmcl.2010.02.084. Epub 2010 Feb 25.

PubMed ID

20227878 [ View in PubMed

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Abstract

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Melatonin	Melatonin receptor type 1A	Ki (nM)	0.296	N/A	N/A	Details
Melatonin	Melatonin receptor type 1B	Ki (nM)	0.429	N/A	N/A	Details