Two distinct classes of novel pyrazolinecarboxamides as potent cannabinoid CB1 receptor agonists |
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| Authors: | Jos H.M. Lange Amos Attali Martina A.W. van der Neut Henri C. Wals Arie Mulder Hicham Zilaout Ate Duursma Hans H.M. van Aken Bernard J. van Vliet |
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| Affiliation: | Abbott Healthcare Products B.V., Chemical Design & Synthesis Unit, C.J. van Houtenlaan 36, 1381 CP Weesp, The Netherlands |
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| Abstract: | 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. |
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