کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1374954 | 981928 | 2006 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
The SAR of 4-substituted (6,6-bicyclic) piperidine cathepsin S inhibitors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
A series of competitive, reversible cathepsin S (CatS) inhibitors was investigated. An earlier disclosure detailed the discovery of the 4-(2-keto-1-benzimidazolinyl)-piperidin-1-yl moiety as an effective replacement for the 4-arylpiperazin-1-yl group found in our screening hit. Continued investigation into replacements for the 4-aryl piperazine resulted in the identification of potentially useful CatS inhibitors with enzymatic and cellular activity similar to that of JNJ 10329670 as disclosed in a previous publication.
Noncovalent, potent, and selective inhibitors of the cysteine protease cathepsin S are reported.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 8, 15 April 2006, Pages 2209–2212
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 8, 15 April 2006, Pages 2209–2212
نویسندگان
Cheryl A. Grice, Kevin Tays, Haripada Khatuya, Darin J. Gustin, Christopher R. Butler, Jianmei Wei, Clark A. Sehon, Siquan Sun, Yin Gu, Wen Jiang, Robin L. Thurmond, Lars Karlsson, James P. Edwards,