کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1373568 | 981903 | 2007 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Identification of a novel class of succinyl-nitrile-based Cathepsin S inhibitors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله

چکیده انگلیسی
The synthesis and in vitro activities of a series of succinyl-nitrile-based inhibitors of Cathepsin S are described. Several members of this class show nanomolar inhibition of the target enzyme as well as cellular potency. The inhibitors displaying the greatest potency contain N-alkyl substituted piperidine and pyrrolidine rings spiro-fused to the α-carbon of the P1 residue.
The synthesis and SAR of the first succinyl-nitrile-based compounds as Cathepsin S inhibitors are described.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 9, 1 May 2007, Pages 2465–2469
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 9, 1 May 2007, Pages 2465–2469
نویسندگان
Younes Bekkali, David S. Thomson, Raj Betageri, Michel J. Emmanuel, Ming-Hong Hao, Eugene Hickey, Weimin Liu, Usha Patel, Yancey D. Ward, Erick R.R. Young, Richard Nelson, Alison Kukulka, Maryanne L. Brown, Kathy Crane, Della White, Dorothy M. Freeman,