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
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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