Article ID Journal Published Year Pages File Type
1374607 Bioorganic & Medicinal Chemistry Letters 2010 7 Pages PDF
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
Physical Sciences and Engineering Chemistry Organic Chemistry
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