Preparation and In Vitro Evaluation of Monoquaternary Inhibitors of Brain Cholinesterases

Author(s): Daniel Jun, Martin Paar, Jiri Binder, Jan Marek, Miroslav Pohanka, Petr Stodulka, Kamil Kuca.

Journal Name: Letters in Organic Chemistry

Volume 6 , Issue 6 , 2009

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Abstract:

Acetylcholinesterase inhibitors are currently of high interest due to the many reasons. Among them, Alzheimers disease drugs are of great interest. In this study, eleven monoquaternary pyridinium salts substituted by different groups (electron donors and electron acceptors) in position four were prepared. Then, their anticholinesterase activity was tested. As observed, their IC50s ranged from 33 μM to 3981 μM. Moreover, probability of blood-brain barrier penetration was predicted.

Keywords: Quaternary ammonium salts, pyridinium salts, inhibitor, cholinesterase, Alzheimer's disease, prophylaxis

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Article Details

VOLUME: 6
ISSUE: 6
Year: 2009
Page: [500 - 503]
Pages: 4
DOI: 10.2174/157017809789124876
Price: $65

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