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

Autor: Lange JH; Abbott Healthcare Products BV, Chemical Design & Synthesis Unit, Weesp, The Netherlands. jos.lange@abbott.com, Attali A, van der Neut MA, Wals HC, Mulder A, Zilaout H, Duursma A, van Aken HH, van Vliet BJ
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Sep 01; Vol. 20 (17), pp. 4992-8. Date of Electronic Publication: 2010 Jul 17.
DOI: 10.1016/j.bmcl.2010.07.056
Abstrakt: 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.
(Copyright 2010 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE
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