کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1366430 | 981590 | 2007 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Optimization of triaryl bis-sulfones as cannabinoid-2 receptor ligands
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Optimization of triaryl bis-sulfones as cannabinoid-2 receptor ligands Optimization of triaryl bis-sulfones as cannabinoid-2 receptor ligands](/preview/png/1366430.png)
چکیده انگلیسی
Structure–activity relationship on our recently reported triaryl bis-sulfone class of cannabinoid-2 (CB2) receptor selective inverse agonists was explored. Modifications to the methane sulfonamide, substitutions to B and C phenyl rings, and replacements of the C-ring were investigated. A compound with excellent CB2 activity, selectivity for CB2 over CB1, and in vivo plasma levels was identified.
Optimization of triaryl bis-sulfone cannabinoid ligands is described. Formation of the trifluoromethane sulfonamide moiety gives compounds that are highly potent and selective for CB2 with improved plasma levels.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 13, 1 July 2007, Pages 3760–3764
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 13, 1 July 2007, Pages 3760–3764
نویسندگان
Brian J. Lavey, Joseph A. Kozlowski, Bandarpalle B. Shankar, James M. Spitler, Guowei Zhou, De-Yi Yang, Youheng Shu, Michael K.C. Wong, Shing-Chun Wong, Neng-Yang Shih, Jie Wu, Stuart W. McCombie, Razia Rizvi, Ronald L. Wolin, Charles A. Lunn,