کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1371623 981849 2010 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Berberine derivatives, with substituted amino groups linked at the 9-position, as inhibitors of acetylcholinesterase/butyrylcholinesterase
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Berberine derivatives, with substituted amino groups linked at the 9-position, as inhibitors of acetylcholinesterase/butyrylcholinesterase
چکیده انگلیسی

Berberine derivatives with substituted amino groups linked at the 9-position using different carbon spacers were designed, synthesized, and biologically evaluated as inhibitors of acetylcholinesterase. Compound 10b, with a cyclohexylamino group linked to berberine by a three carbon spacer, gave the most potent inhibitor activity with an IC50 of 0.020 μM for AChE. Kinetic studies revealed mixed inhibition of AChE, and molecular modeling simulations of the AChE–inhibitor complex confirmed that compounds bound to both the catalytic active site and the peripheral anionic site.

Berberine derivatives with substituted amino groups linked on the 9-position of berberine with different carbon spacers were designed, synthesized, and biologically evaluated as inhibitors of acetylcholinesterase. Compound 10b with a cyclohexylamino group linked to berberine by a three carbon spacer, gave the most potent inhibitor activity with an IC50 value of 0.020 μM for AchE.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 22, 15 November 2010, Pages 6649–6652
نویسندگان
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