کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1373500 981898 2007 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors
چکیده انگلیسی

This Letter describes the design and synthesis of tertiary carbinamine macrocyclic inhibitors of the β-secretase (BACE-1) enzyme. These macrocyclic inhibitors, some of which incorporate novel P2 substituents, display a 2- to 100-fold increase in potency relative to the previously described acyclic analogs while affording greater stability.

This Letter describes the design and synthesis of tertiary carbinamine macrocyclic inhibitors of the β-secretase (BACE-1) enzyme. These macrocyclic inhibitors, some of which incorporate novel P2 substituents, display a 2- to 100-fold increase in potency relative to the previously described acyclic analogs while affording greater stability.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 14, 15 July 2007, Pages 4057–4061
نویسندگان
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