کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1366394 981590 2007 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Discovery of 6-ethyl-2,4-diaminopyrimidine-based small molecule renin inhibitors
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Discovery of 6-ethyl-2,4-diaminopyrimidine-based small molecule renin inhibitors
چکیده انگلیسی

Novel 2,4-diaminopyrimidine-based small molecule renin inhibitors are disclosed. Through high throughput screening, parallel synthesis, X-ray crystallography, and structure based drug design, we have developed the first non-chiral, non-peptidic, small molecular template to possess moderate potency against renin. The designed compounds consist of a novel 6-ethyl-5-(1,2,3,4-tetrahydroquinolin-7-yl)pyrimidine-2,4-diamine ring system that exhibit moderate potency (IC50: 91–650 nM) against renin while remaining ‘Rule-of-five’ compliant.

Novel 2,4-diaminopyrimidine-based small molecule renin inhibitors are disclosed. Through high throughput screening, parallel synthesis, X-ray crystallography, and structure based drug design, we have developed the first non-chiral, non-peptidic, small molecular template to possess moderate potency against renin. The designed compounds consist of a novel 6-ethyl-5-(1,2,3,4-tetrahydroquinolin-7-yl)pyrimidine-2,4-diamine ring system that exhibit moderate potency (IC50: 91–650 nM) against renin while remaining ‘Rule-of-five’ compliant.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 13, 1 July 2007, Pages 3575–3580
نویسندگان
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