3-(4-Piperidinyl)indoles and 3-(4-piperidinyl)pyrrolo-[2,3-b]pyridines as ligands for the ORL-1 receptor.

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作者信息

Bignan Gilles C, Battista Kathleen, Connolly Peter J, Orsini Michael J, Liu Jingchun, Middleton Steven A, Reitz Allen B

机构信息

Johnson & Johnson Pharmaceutical Research and Development, L.L.C PO Box 300, 1000 Route 202, Raritan, NJ 08869, USA.

出版信息

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3524-8. doi: 10.1016/j.bmcl.2006.03.094. Epub 2006 Apr 24.

DOI:10.1016/j.bmcl.2006.03.094

PMID:16632355

Abstract

A novel series of indoles and 1H-pyrrolo[2,3-b]pyridines having a piperidine ring at the 3-position were synthesized and found to bind with high affinity to the ORL-1 receptor. Structure-activity relationships at the piperidine nitrogen were investigated in each series. Substitution on the phenyl ring and nitrogen atom of the indole and 1H-pyrrolo[2,3-b]pyridine cores generated several selective high-affinity ligands that were agonists of the ORL-1 receptor.

摘要

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