کد مقاله کد نشریه سال انتشار مقاله انگلیسی ترجمه فارسی نسخه تمام متن
1368627 981704 2016 3 صفحه PDF ندارد دانلود رایگان
عنوان انگلیسی مقاله
Design, synthesis and bioactivity of novel phthalimide derivatives as acetylcholinesterase inhibitors
ترجمه فارسی عنوان
طراحی، سنتز و فعالیت زیستی مشتقات فتالیمید جدید به عنوان مهارکننده های آنزیم استیل کولین استراز
کلمات کلیدی
ترکیبی زیربنا؛ مشتقات فتالیمید؛ مهارکننده آنزیم استیل کولین استراز. رابطه ساختار فعالیت؛ داکینگ مولکولی
Substructure combination; Phthalimide derivatives; Acetylcholinesterase inhibitor; Structure–activity relationship; Molecular docking
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی

A series of novel phthalimide derivatives related to benzylpiperazine were synthesized and evaluated as cholinesterase inhibitors. The results showed that all compounds were able to inhibit acetylcholinesterase (AChE), with two of them dramatically inhibiting butyrylcholinesterase (BuChE). Most compounds exhibited potent anti-AChE activity in the range of nM concentrations. In particular, compounds 7aIII and 10a showed the most potent activity with the IC50 values of 18.44 nM and 13.58 nM, respectively. To understand the excellent activity of these compounds, the structure–activity relationship was further examined. The protein–ligand docking study demonstrated that the target compounds have special binding modes and these results are in agreement with the kinetic study.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 9, 1 May 2016, Pages 2380–2382
نویسندگان
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