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
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
The SAR of 4-substituted (6,6-bicyclic) piperidine cathepsin S inhibitors
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
نویسندگان
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