کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1375144 | 981932 | 2010 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Identification of SD-0006, a potent diaryl pyrazole inhibitor of p38 MAP kinase
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Starting from an initial HTS screening lead, a novel series of C(5)-substituted diaryl pyrazoles were developed that showed potent inhibition of p38α kinase. Key to this outcome was the switch from a pyridyl to pyrimidine at the C(4)-position leading to analogs that were potent in human whole blood based cell assay as well as in a number of animal efficacy models for rheumatoid arthritis. Ultimately, we identified a clinical candidate from this substrate; SD-0006.
Starting from the novel screening lead, SC-102, synthesis and structure activity relationships are provided highlighting the progression to and identification of the potent p38 MAP kinase inhibitor SD-0006.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 8, 15 April 2010, Pages 2634–2638
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 8, 15 April 2010, Pages 2634–2638
نویسندگان
John K. Walker, Shaun R. Selness, Rajesh V. Devraj, Michael E. Hepperle, Win Naing, Huey Shieh, Ravi Kurambail, Syaulan Yang, Daniel L. Flynn, Alan G. Benson, Dean M. Messing, Tom Dice, Tina Kim, R.J. Lindmark, Joseph B. Monahan, Joseph Portanova,