Two distinct classes of novel pyrazolinecarboxamides as potent cannabinoid CB1 receptor agonists
| Autor: | Hicham Zilaout, Hans van Aken, Henri C. Wals, Amos Attali, Arie H. Mulder, Martina A.W. van der Neut, Vliet Bernard J Van, Josephus H. M. Lange, Ate Duursma |
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| Rok vydání: | 2010 |
| Předmět: |
Agonist
Cannabinoid receptor medicine.drug_class Chemistry medicine.medical_treatment Organic Chemistry Clinical Biochemistry Pharmaceutical Science Pharmacology Biochemistry Chemical synthesis In vitro Receptor Cannabinoid CB1 In vivo Oral administration Drug Discovery medicine Molecular Medicine Pyrazoles Cannabinoid Receptor Molecular Biology |
| Zdroj: | Bioorganicmedicinal chemistry letters. 20(17) |
| ISSN: | 1464-3405 |
| Popis: | 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 CB(1) receptor agonist classes were described. The target compounds elicited high affinities to the CB(1) as well as the CB(2) receptor and were found to act as CB(1) receptor agonists. The key compound 19 elicited potent CB(1) agonistic and CB(2) inverse agonistic properties in vitro and showed in vivo activity in a rodent model for multiple sclerosis after oral administration. |
| Databáze: | OpenAIRE |
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