Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1374607 | Bioorganic & Medicinal Chemistry Letters | 2010 | 7 Pages |
Abstract
The synthesis and SAR of 3-alkyl-4-aryl-4,5-dihydropyrazole-1-carboxamides 1–23 and 1-alkyl-5-aryl-4,5-dihydropyrazole-3-carboxamides 24–27 as two novel cannabinoid CB1 receptor agonist classes were described. The target compounds elicited high affinities to the CB1 as well as the CB2 receptor and were found to act as CB1 receptor agonists. The key compound 19 elicited potent CB1 agonistic and CB2 inverse agonistic properties in vitro and showed in vivo activity in a rodent model for multiple sclerosis after oral administration.
Graphical abstractThe synthesis and SAR of two novel CB1 receptor agonist classes A and B are described.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
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Organic Chemistry
Authors
Jos H.M. Lange, Amos Attali, Martina A.W. van der Neut, Henri C. Wals, Arie Mulder, Hicham Zilaout, Ate Duursma, Hans H.M. van Aken, Bernard J. van Vliet,