New 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides were synthesized as cannabinoid (CB) receptor ligands. Compound 11 (CB 1 K i = 2.3 nM, CB 1 SI = 163.6) showed CB 1 receptor affinity and selectivity superior to Rimonabant and AM251. Acute administration of 2 mg/kg 11 reduced sucrose, but not regular food, intake in rats. On the other hand, compound 23 (CB 2 K i = 0.51 nM, CB 2 SI = 30.0) showed significant affinity and selectivity for the CB 2 receptor. The results presented here show that the 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3- carboxamide may serve as an effective scaffold for the design of either CB 1 or CB 2 receptor ligands. © 2011 Elsevier Masson SAS. All rights reserved.
Piscitelli, F., Ligresti, A., LA REGINA, G., Gatti, V., Brizzi, A., Pasquini, S., et al. (2011). 1-Aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamide: An effective scaffold for the design of either CB1 and CB2 receptor ligands. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 46(11), 5641-5653 [10.1016/j.ejmech.2011.09.037].
1-Aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamide: An effective scaffold for the design of either CB1 and CB2 receptor ligands
GATTI V.;BRIZZI A.;PASQUINI S.;CORELLI F.;
2011-01-01
Abstract
New 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides were synthesized as cannabinoid (CB) receptor ligands. Compound 11 (CB 1 K i = 2.3 nM, CB 1 SI = 163.6) showed CB 1 receptor affinity and selectivity superior to Rimonabant and AM251. Acute administration of 2 mg/kg 11 reduced sucrose, but not regular food, intake in rats. On the other hand, compound 23 (CB 2 K i = 0.51 nM, CB 2 SI = 30.0) showed significant affinity and selectivity for the CB 2 receptor. The results presented here show that the 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3- carboxamide may serve as an effective scaffold for the design of either CB 1 or CB 2 receptor ligands. © 2011 Elsevier Masson SAS. All rights reserved.
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https://hdl.handle.net/11365/20296
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