کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1367827 | 981650 | 2005 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Triaryl bis-sulfones as cannabinoid-2 receptor ligands: SAR studies
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
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چکیده انگلیسی
We recently reported that compound 1 is a potent inhibitor of the CB2 receptor with high selectivity over CB1. This paper describes the SAR development for this class of compounds. Variation of the substitution pattern on the aromatic rings, as well as the groups linking them together, led to sub-nanomolar inhibitors of the CB2 receptor, with high selectivity over CB1.
SAR studies on recently reported triaryl bis-sulfone cannabinoid CB2 receptor ligands are described. Modification of aryl substitution and their respective linkers gives compounds that are highly potent and selective for CB2. One compound is shown to be an orally available CB2-selective inverse agonist.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 20, 15 October 2005, Pages 4417–4420
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 20, 15 October 2005, Pages 4417–4420
نویسندگان
Bandarpalle B. Shankar, Brian J. Lavey, Guowei Zhou, James A. Spitler, Ling Tong, Razia Rizvi, De-Yi Yang, Ronald Wolin, Joseph A. Kozlowski, Neng-Yang Shih, Jie Wu, R. William Hipkin, Waldemar Gonsiorek, Charles A. Lunn,