کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10595451 981862 2013 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Exploration of the 5-bromopyrimidin-4(3H)-ones as potent inhibitors of PDE5
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Exploration of the 5-bromopyrimidin-4(3H)-ones as potent inhibitors of PDE5
چکیده انگلیسی
The substituents both at the 6-position of the 5-bromopyrimidinone ring and at the 5′-position of the phenyl ring of 5-bromopyrimidin-4(3H)-ones were explored. 5-Bromo-6-isopropyl-2-(2-propoxy-phenyl)pyrimidin-4(3H)-one was identified as a new scaffold for potent PDE5 inhibitors. The crystal structures of PDE5/2e and PDE5/10a complexes provided a structural basis for the inhibition of 5-bromopyrimidinones to PDE5. In addition, it was also found that there is a great tolerance for the substitution at the 5′-position of the phenyl ring of 5-bormopyrimidinones and the resulted compound 13a has the highest inhibition activity to PDE5 (IC50, 1.7 nM).
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 17, 1 September 2013, Pages 4944-4947
نویسندگان
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