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Bioorg Med Chem Lett. 2008 Jul 1;18(13):3778-82. doi: 10.1016/j.bmcl.2008.05.036. Epub 2008 May 16.

Design, synthesis, and structure-activity relationship study of a novel class of ORL1 receptor antagonists based on N-biarylmethyl spiropiperidine.

Author information

1
Tsukuba Research Institute, Banyu Pharmaceutical Co. Ltd, Okubo-3, Tsukuba 300-2611, Ibaraki, Japan. takashi_yoshizumi@merck.com

Abstract

Based on reported structures, a focused library of biarylmethyl bound to the nitrogen atom of spiropiperidine was designed. Systematic modifications allowed the discovery of a synthetically feasible and highly potent ORL1 antagonist 37, 1'-{[1-(3-chloropyridin-2-yl)-1H-pyrazol-4-yl]methyl}-3H-spiro[2-benzofuran-1,4'-piperidine], which exhibits excellent selectivity to mu, kappa, and human ether-a-go-go related gene potassium channel.

PMID:
18515099
DOI:
10.1016/j.bmcl.2008.05.036
[Indexed for MEDLINE]

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