کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1364112 | 981529 | 2007 | 38 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
We report the design and synthesis of a series of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as orally bioavailable small molecule inhibitors of renin. Compounds with a 2-methyl-2-aryl substitution pattern exhibit potent renin inhibition and good permeability, solubility, and metabolic stability. Oral bioavailability was found to be dependent on metabolic clearance and cellular permeability, and was optimized through modulation of the sidechain that binds in the S3sp subsite.
We report the design and synthesis of a series of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones that are orally bioavailable small molecule inhibitors of renin.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 15, Issue 17, 1 September 2007, Pages 5912–5949
Journal: Bioorganic & Medicinal Chemistry - Volume 15, Issue 17, 1 September 2007, Pages 5912–5949
نویسندگان
Noel A. Powell, Fred L. Ciske, Cuiman Cai, Daniel D. Holsworth, Ken Mennen, Chad A. Van Huis, Mehran Jalaie, Jacqueline Day, Michelle Mastronardi, Pat McConnell, Igor Mochalkin, Erli Zhang, Michael J. Ryan, John Bryant, Wendy Collard, Suzie Ferreira,