کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1362808 981496 2005 8 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Design and synthesis of N-benzylpiperidine–purine derivatives as new dual inhibitors of acetyl- and butyrylcholinesterase
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Design and synthesis of N-benzylpiperidine–purine derivatives as new dual inhibitors of acetyl- and butyrylcholinesterase
چکیده انگلیسی

The synthesis and biological evaluation of N-benzyl-(piperidin or pyrrolidin)-purines are described. Compounds derived from N-benzylpiperidine and N-substituted purines showed moderate acetylcholinesterase inhibition. Preliminary structure–activity relationships and a superimposition of the best compound with the active conformation of donepezil have revealed structural features that have been used in the design of more potent N-benzylpiperidine inhibitors bearing an 8-substituted caffeine fragment and a methoxymethyl linker. These new compounds are interesting dual inhibitors of acetylcholinesterase and butyrylcholinesterase and have been chosen for further optimisation.

The synthesis of new N-benzylpiperidine–purine derivatives and their dual inhibition of acetyl- and butyrylcholinesterase are presented.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 13, Issue 24, 15 December 2005, Pages 6795–6802
نویسندگان
, , , , ,