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

被引：15

作者：

Bignan, Gilles C.

Battista, Kathleen

Connolly, Peter J.

Liu, Jingchun

Middleton, Steven A.

Reitz, Allen B.

机构：

[1] Johnson & Johnson Pharmaceut Res & Dev LLC, Raritan, NJ 08869 USA

[2] Johnson & Johnson Pharmaceut Res & Dev LLC, Spring House, PA 19477 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 13期

关键词：

ORL-1; nociceptin; opioid receptor-like (ORL); orphanin FQ (OFQ); N/OFQ peptide (NOP); agonist; indole; piperidine; pyridine; anxiety; stress; learning; memory;

D O I：

10.1016/j.bmcl.2006.03.094

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：3524 / 3528

页数：5

共 30 条

[1] Preparation of 3-spirocyclic indolin-2-ones as ligands for the ORL-1 receptor [J].