کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10588264 | 981450 | 2011 | 12 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis, biological evaluation and docking studies of octane-carboxamide based renin inhibitors with extended segments toward S3â² site of renin
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Eighteen octane-carboxamide based renin inhibitors with extended segments for mimicking P3â² unit of angiotensinogen have been synthesized. The biological evaluation identified novel renin inhibitors with more potent activity than aliskiren. Molecular docking studies showed that the extended amide-tails matched the P3â² position of angiotensinogen and exerted interactions with the S3â² site of renin. An unexpected Ï-Ï stacking interaction was observed during docking study for compound 9r, which could be a reasonable explanation for the outstanding potency of this compound. Further study is in progress to reveal a feasibility for developing novel renin inhibitors based on the possible non-classical interactions between the ligands and the new subsite of renin.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 14, 15 July 2011, Pages 4238-4249
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 14, 15 July 2011, Pages 4238-4249
نویسندگان
Yong Wu, Chen Shi, Xiaowei Sun, Xiaoming Wu, Hongbin Sun,