کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1367658 981641 2006 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
New bicyclic cannabinoid receptor-1 (CB1-R) antagonists
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
New bicyclic cannabinoid receptor-1 (CB1-R) antagonists
چکیده انگلیسی

A series of conformationally constrained bicyclic derivatives derived from SR141716 was prepared and evaluated as hCB1-R antagonists and inverse agonists. Optimization of the structure–activity relationships around the 2,6-dihydro-pyrazolo[4,3-d]pyrimidin-7-one derivative 2a led to the identification of two compounds with oral activity in rodent feeding models (2h and 4a). Replacement of the PP group in 2h with other bicyclic groups resulted in a loss of binding affinity.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 3, 1 February 2006, Pages 731–736
نویسندگان
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