期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 46, 期 11, 页码 5641-5653出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2011.09.037
关键词
Cannabinoid; Human recombinant CB receptor type 1; Pyrrole bioisosteres; Structure-activity relationships; Pharmacological studies
New 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides were synthesized as cannabinoid (CB) receptor ligands. Compound 11 (CB1 K-i = 2.3 nM, CB1 SI = 163.6) showed CB1 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 (CB2 K-i = 0.51 nM, CB2 SI =30.0) showed significant affinity and selectivity for the CB2 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 CB1 or CB2 receptor ligands. (C) 2011 Elsevier Masson SAS. All rights reserved.
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