کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1374607 | 981922 | 2010 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Two distinct classes of novel pyrazolinecarboxamides as potent cannabinoid CB1 receptor agonists
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
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.
The synthesis and SAR of two novel CB1 receptor agonist classes A and B are described.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 17, 1 September 2010, Pages 4992–4998
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 17, 1 September 2010, Pages 4992–4998
نویسندگان
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,