کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1370706 | 981827 | 2015 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of novel pyrazole-containing benzamides as potent RORγ inverse agonists
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The nuclear receptor RORγ plays a central role in controlling a pro-inflammatory gene expression program in several lymphocyte lineages including TH17 cells. RORγ-dependent inflammation has been implicated in the pathogenesis of several major autoimmune diseases and thus RORγ is an attractive target for therapeutic intervention in these diseases. Starting from a lead biaryl compound 4a, replacement of the head phenyl moiety with a substituted aminopyrazole group resulted in a series with improved physical properties. Further SAR exploration led to analogues (e.g., 4j and 5m) as potent RORγ inverse agonists.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 25, Issue 15, 1 August 2015, Pages 2985–2990
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 25, Issue 15, 1 August 2015, Pages 2985–2990
نویسندگان
Tao Wang, Daliya Banerjee, Tonika Bohnert, Jianhua Chao, Istvan Enyedy, Jason Fontenot, Kevin Guertin, Howard Jones, Edward Y. Lin, Douglas Marcotte, Tina Talreja, Kurt Van Vloten,