کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1373388 | 1500544 | 2010 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design, synthesis, and structure–activity relationship study of bicyclic piperazine analogs of indole-3-carboxamides as novel cannabinoid CB1 receptor agonists
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Design, synthesis, and structure–activity relationship study of bicyclic piperazine analogs of indole-3-carboxamides as novel cannabinoid CB1 receptor agonists Design, synthesis, and structure–activity relationship study of bicyclic piperazine analogs of indole-3-carboxamides as novel cannabinoid CB1 receptor agonists](/preview/png/1373388.png)
چکیده انگلیسی
Bicyclic piperazine derivatives were synthesized as conformationally constrained analogs of N-alkyl piperazines and were found to be potent CB1 receptor agonists. The CB1 receptor agonist activity was dependent upon the absolute configuration of the chiral center of the bicyclic ring system. Although the conformational constraint did not protect the compounds from metabolism by N-dealkylation, several bicyclic analogs were found to be more potent than the unconstrained lead compound. Compound 8b demonstrated potent antinociceptive activity in vivo.
Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 24, 15 December 2010, Pages 7327–7330
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 24, 15 December 2010, Pages 7327–7330
نویسندگان
Elizabeth M. Moir, Kazuya Yoshiizumi, Jim Cairns, Phillip Cowley, Morag Ferguson, Fiona Jeremiah, Takao Kiyoi, Richard Morphy, Jason Tierney, Grant Wishart, Mark York, James Baker, Jean E. Cottney, Andrea K. Houghton, Petula McPhail, Andrew Osprey,