کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1372084 | 981865 | 2010 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Piperidine-based heterocyclic oxalyl amides as potent p38α MAP kinase inhibitors
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The design and synthesis of a new class of p38α MAP kinase inhibitors based on 4-fluorobenzylpiperidine heterocyclic oxalyl amides are described. Many of these compounds showed low-nanomolar activities in p38α enzymatic and cell-based cytokine TNFα production inhibition assays. The optimal linkers between the piperidine and the oxalyl amide were found to be [6,5] fused ring heterocycles. Substituted indoles and azaindoles were favored structural motifs in the cellular assay.
A new class of p38α MAP kinase inhibitors based on 4-fluorobenzylpiperidine substituted heterocycles is described. Optimal features include a piperidine and an oxalyl amide separated by a [6,5] fused ring heterocycle.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 3, 1 February 2010, Pages 1059–1062
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 3, 1 February 2010, Pages 1059–1062
نویسندگان
Babu J. Mavunkel, John J. Perumattam, Xuefei Tan, Gregory R. Luedtke, Qing Lu, Don Lim, Darin Kizer, Sundeep Dugar, Sarvajit Chakravarty, Yong-jin Xu, Joon Jung, Albert Liclican, Daniel E. Levy, Jocelyn Tabora,