کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1372960 | 981886 | 2011 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design, synthesis and activity of a potent, selective series of N-aryl pyridinone inhibitors of p38 kinase
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A series of N-aryl pyridinone inhibitors of p38 mitogen activated protein (MAP) kinase were designed and prepared based on the screening hit SC-25028 (1) and structural comparisons to VX-745 (5). The focus of the investigation targeted the dependence of potency and metabolic stability on the benzyloxy connectivity, the role of the C-6 position and the substitution pattern on the N-phenyl ring. Further optimization produced the highly selective and potent pyridinones 2 and 3. These inhibitors exhibited activity in both acute and chronic models of inflammation.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 13, 1 July 2011, Pages 4059–4065
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 13, 1 July 2011, Pages 4059–4065
نویسندگان
Shaun R. Selness, Terri L. Boehm, John K. Walker, Balekudru Devadas, Richard C. Durley, Ravi Kurumbail, Huey Shieh, Li Xing, Michael Hepperle, Paul V. Rucker, Kevin D. Jerome, Alan G. Benson, Laura D. Marrufo, Heather M. Madsen, Jeff Hitchcock,