Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1373388 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
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.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Elizabeth M. Moir, Kazuya Yoshiizumi, Jim Cairns, Phillip Cowley, Morag Ferguson, Fiona Jeremiah, Takao Kiyoi, Richard Morphy, Jason Tierney, Grant Wishart, Mark York, James Baker, Jean E. Cottney, Andrea K. Houghton, Petula McPhail, Andrew Osprey,