کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1374558 | 981921 | 2010 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design and optimization of a substituted amino propanamide series of renin inhibitors for the treatment of hypertension
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The discovery and SAR of a new series of substituted amino propanamide renin inhibitors are herein described. This work has led to the preparation of compounds with in vitro and in vivo profiles suitable for further development. Specifically, challenges pertaining to oral bioavailability, covalent binding and time-dependent CYP 3A4 inhibition were overcome thereby culminating in the identification of compound 50 as an optimized renin inhibitor with good efficacy in the hypertensive double-transgenic rat model.
The design and synthesis of orally bioavailable, potent acyclic renin inhibitors are described therein.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 7, 1 April 2010, Pages 2204–2209
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 7, 1 April 2010, Pages 2204–2209
نویسندگان
Austin Chen, Christopher Bayly, Olivier Bezençon, Sylvia Richard-Bildstein, Daniel Dubé, Laurence Dubé, Sébastien Gagné, Michel Gallant, Mireille Gaudreault, Erich Grimm, Robert Houle, Patrick Lacombe, Sébastien Laliberté, Jean-François Lévesque,