کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1373029 | 981888 | 2008 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
α,β-Cyclic-β-benzamido hydroxamic acids: Novel oxaspiro[4.4]nonane templates for the discovery of potent, selective, orally bioavailable inhibitors of tumor necrosis factor-α converting enzyme (TACE)
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: α,β-Cyclic-β-benzamido hydroxamic acids: Novel oxaspiro[4.4]nonane templates for the discovery of potent, selective, orally bioavailable inhibitors of tumor necrosis factor-α converting enzyme (TACE) α,β-Cyclic-β-benzamido hydroxamic acids: Novel oxaspiro[4.4]nonane templates for the discovery of potent, selective, orally bioavailable inhibitors of tumor necrosis factor-α converting enzyme (TACE)](/preview/png/1373029.png)
چکیده انگلیسی
Two novel oxaspiro[4.4]nonane β-benzamido hydroxamic scaffolds have been synthesized in enantio- and diasteriomerically pure form. These templates proved to be exceptional platforms that have led to the discovery of potent inhibitors of TACE that are active in a cellular assay measuring suppression of LPS-induced TNF-α. Furthermore, these inhibitors are selective against related MMPs, demonstrate permeability in a Caco-2 assay, and display good oral bioavailability.
Selective inhibitors of TNF-α Converting Enzyme (TACE) based on novel oxaspiro[4.4]nonane β-benzamido hydroxamic scaffolds acids have been synthesized and evaluated.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 4, 15 February 2008, Pages 1288–1292
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 4, 15 February 2008, Pages 1288–1292
نویسندگان
Gregory R. Ott, Naoyuki Asakawa, Rui-Qin Liu, Maryanne B. Covington, Mingxin Qian, Krishna Vaddi, Robert C. Newton, James M. Trzaskos, David D. Christ, Laurine Galya, Thomas Scholz, Will Marshall, James J.-W. Duan,