个性化文献订阅>期刊> Bioorganic & Medicinal Chemistry Letters
 

Two distinct classes of novel pyrazolinecarboxamides as potent cannabinoid CB1 receptor agonists

  作者 Lange, JHM; Attali, A; van der Neut, MAW; Wals, HC; Mulder, A; Zilaout, H; Duursma, A; van Aken, HHM; van Vliet, BJ  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2010年20-17;  页码  4992-4998  
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[摘要]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. (C) 2010 Elsevier Ltd. All rights reserved.

 
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