کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1371362 | 981843 | 2010 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Optimization of α-ketoamide based p38 inhibitors through modifications to the region that binds to the allosteric site
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
We have optimized a novel series of potent p38 MAP kinase inhibitors based on an α-ketoamide scaffold through structure based design that due to their extended molecular architecture bind, in addition to the ATP site, to an allosteric pocket. In vitro ADME, in vivo PK and efficacy studies show these compounds to have drug-like characteristics and have resulted in the nomination of a development candidate which is currently in phase II clinical trials for the oral treatment of inflammatory conditions.
The design and synthesis of novel α-ketoamide based p38 inhibitors is reported.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 16, 15 August 2010, Pages 4819–4824
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 16, 15 August 2010, Pages 4819–4824
نویسندگان
Antonio Garrido Montalban, Erik Boman, Chau-Dung Chang, Susana Conde Ceide, Russell Dahl, David Dalesandro, Nancy G.J. Delaet, Eric Erb, Justin T. Ernst, Andrew Gibbs, Jeffrey Kahl, Linda Kessler, Jeff Kucharski, Christopher Lum, Jan Lundström,