کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1370908 981833 2011 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Difluoroethylamines as an amide isostere in inhibitors of cathepsin K
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Difluoroethylamines as an amide isostere in inhibitors of cathepsin K
چکیده انگلیسی

The trifluoroethylamine group found in cathepsin K inhibitors like odanacatib can be replaced by a difluoroethylamine group. This change increased the basicity of the nitrogen which positively impacted the log D. This translated into an improved oral bioavailability in pre-clinical species. Difluoroethylamine compounds exhibit a similar potency against cathepsin K and selectivity profile against other cathepsins when compared to trifluoroethylamine analogs.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 3, 1 February 2011, Pages 920–923
نویسندگان
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