☆ 4.7 Article

Structure-activity relationships and CoMFA of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic properties

BIOORGANIC & MEDICINAL CHEMISTRY (2008)

期刊

BIOORGANIC & MEDICINAL CHEMISTRY

卷 16, 期 6, 页码 2829-2851

出版社

PERGAMON-ELSEVIER SCIENCE LTD

DOI: 10.1016/j.bmc.2008.01.005

关键词

NOP/ORL1 agonist; antinociception; antiallodynia; pain; CoMFA model

类别

Biochemistry & Molecular Biology Chemistry, Medicinal Chemistry, Organic

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摘要

The N-3 position of a series of 3-phenoxypropyl piperidine benzimidazol-2-one analogues was optimised using the predictive power of a CoMFA model. The model was used to prioritise compounds for synthesis culminating in the triazole (+)-24. (+)-24 was found to be a high affinity, potent NOP agonist and demonstrated both antinociceptive and antiallodynic effects when administered iv to rodents. (C) 2008 Elsevier Ltd. All rights reserved.

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