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
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله

چکیده انگلیسی
The substituents both at the 6-position of the 5-bromopyrimidinone ring and at the 5â²-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 5â²-position of the phenyl ring of 5-bormopyrimidinones and the resulted compound 13a has the highest inhibition activity to PDE5 (IC50, 1.7Â nM).
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 17, 1 September 2013, Pages 4944-4947
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 17, 1 September 2013, Pages 4944-4947
نویسندگان
Xudong Gong, Guan Wang, Jing Ren, Zheng Liu, Zhen Wang, Tiantian Chen, Xiaojun Yang, Xiangrui Jiang, Jingshan Shen, Hualiang Jiang, Haji Akber Aisa, Yechun Xu, Jianfeng Li,