کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1372622 | 981872 | 2009 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Novel carbamate cholinesterase inhibitors that release biologically active amines following enzyme inhibition
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Conjugation of the phenol derived from rivastigmine with amphetamines gave access to novel carbamate cholinesterase inhibitors. All compounds possessed increased affinity and selectivity for AChE compared to rivastigmine and were orally bioavailable. Compound 4a, incorporating d-amphetamine, caused significant inhibition of cholinesterase in vivo at doses that were well tolerated. Release of amphetamine from 4a was demonstrated following in vitro and in vivo inhibition of cholinesterase. Compound 4a was also effective in alleviating scopolamine induced amnesia in a rat passive avoidance model.
Upon inhibition of cholinesterase by 4a–d, pharmacologically active amines are released.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 12, 15 June 2009, Pages 3243–3246
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 12, 15 June 2009, Pages 3243–3246
نویسندگان
Jeroen C. Verheijen, Kjesten A. Wiig, Shoucheng Du, Stacie L. Connors, Ashley N. Martin, Jennifer P. Ferreira, Vladimir I. Slepnev, Ulrike Kochendörfer,