کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1362519 | 981490 | 2010 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The trifluoromethylphenyl P2 motif from previously reported heteroarylnitrile series has been successfully applied for the design and synthesis of highly potent novel ketoamide-based cathepsin S inhibitors. The key in this process is the change of the torsion angle between the P2 phenyl ring and the attached secondary amide by adding a small Cl, F, or Me group at the 2-position.
By using a small atom (Cl, F, or Me) to increase the torsion angle between the phenyl ring and the attached secondary amide, trifluoromethylphenyl motif was applied successfully as P2 for aldehyde/ketoamide-based cathepsin S inhibitors.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 23, 1 December 2010, Pages 6890–6894
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 23, 1 December 2010, Pages 6890–6894
نویسندگان
Jiaqiang Cai, John Robinson, Simone Belshaw, Kathryn Everett, Xavier Fradera, Mario van Zeeland, Leon van Berkom, Peter van Rijnsbergen, Lucy Popplestone, Mark Baugh, Maureen Dempster, John Bruin, William Hamilton, Emma Kinghorn, Paul Westwood,