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Tricyclic Pyrazole-Based Compounds as Useful Scaffolds for Cannabinoid $CB_{1}/CB_{2}$ Receptor Interaction
| Content Provider | MDPI |
|---|---|
| Author | Asproni, Battistina Murineddu, Gabriele Corona, Paola Pinna, Gérard |
| Copyright Year | 2021 |
| Description | Cannabinoids comprise different classes of compounds, which aroused interest in recent years because of their several pharmacological properties. Such properties include analgesic activity, bodyweight reduction, the antiemetic effect, the reduction of intraocular pressure and many others, which appear correlated to the affinity of cannabinoids towards CB1 and/or CB2 receptors. Within the search aiming to identify novel chemical scaffolds for cannabinoid receptor interaction, the CB1 antagonist/inverse agonist pyrazole-based derivative rimonabant has been modified, giving rise to several tricyclic pyrazole-based compounds, most of which endowed of high affinity and selectivity for CB1 or CB2 receptors. The aim of this review is to present the synthesis and summarize the SAR study of such tricyclic pyrazole-based compounds, evidencing, for some derivatives, their potential in the treatment of neuropathic pain, obesity or in the management of glaucoma. |
| Starting Page | 2126 |
| e-ISSN | 14203049 |
| DOI | 10.3390/molecules26082126 |
| Journal | Molecules |
| Issue Number | 8 |
| Volume Number | 26 |
| Language | English |
| Publisher | MDPI |
| Publisher Date | 2021-04-07 |
| Access Restriction | Open |
| Subject Keyword | Molecules Medicinal Chemistry Tricyclic Pyrazoles Structure-activity Relationship Cb2 Agonist Cb1 Agonist Cb1 Neutral Antagonist Anti-nociceptive Activity Glaucoma Obesity |
| Content Type | Text |
| Resource Type | Article |