☆ 4.5 Article

Identification of 3-substituted N-benzhydryl-nortropane analogs as nociceptin receptor ligands for the management of cough and anxiety

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2009)

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷 19, 期 9, 页码 2482-2486

出版社

PERGAMON-ELSEVIER SCIENCE LTD

DOI: 10.1016/j.bmcl.2009.03.057

关键词

Nociceptin; Antitussive; Anxiolytic; NOP

类别

Chemistry, Medicinal Chemistry, Organic

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摘要

A series of nortropane analogs based on previously reported compound 1 have been synthesized and shown to bind to the nociceptin receptor with high affinity. The synthesis and structure-activity relationships around the C-3 nortropane substitution are described. From the SAR study and hPXR screening effort, compound 15 was identified to possess potent oral antitussive and anxiolytic-like activities in the guinea pig models. (c) 2009 Elsevier Ltd. All rights reserved.

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