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

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

A series of substituted N-[3-(3-methoxyphenyl)propyl] amides were synthesized and their binding affinities towards human melatonin MT sub(1) and MT sub(2) receptors were evaluated. It was discovered that a benzyloxyl substituent incorporated at C6 position of the 3-methoxyphenyl ring dramatically en...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2010-04, Vol.20 (8), p.2582-2585
Hauptverfasser: Hu, Yueqing, Ho, Maurice KC, Chan, King H, New, David C, Wong, Yung H
Format: Artikel
Sprache:eng
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Zusammenfassung:A series of substituted N-[3-(3-methoxyphenyl)propyl] amides were synthesized and their binding affinities towards human melatonin MT sub(1) and MT sub(2) receptors were evaluated. It was discovered that a benzyloxyl substituent incorporated at C6 position of the 3-methoxyphenyl ring dramatically enhanced the MT sub(2) binding affinity and at the same time decreased MT sub(1) binding affinity.
ISSN:0960-894X
DOI:10.1016/j.bmcl.2010.02.084