期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 24, 页码 7327-7330出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.10.061
关键词
Cannabinoid CB1 receptor; GPCR agonist
Bicyclic piperazine derivatives were synthesized as conformationally constrained analogs of N-alkyl piperazines and were found to be potent CB1 receptor agonists. The CB1 receptor agonist activity was dependent upon the absolute configuration of the chiral center of the bicyclic ring system. Although the conformational constraint did not protect the compounds from metabolism by N-dealkylation, several bicyclic analogs were found to be more potent than the unconstrained lead compound. Compound 8b demonstrated potent antinociceptive activity in vivo. (C) 2010 Elsevier Ltd. All rights reserved.
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