Preparation and In Vitro Evaluation of Monoquaternary Inhibitors of Brain Cholinesterases

Title: Preparation and In Vitro Evaluation of Monoquaternary Inhibitors of Brain Cholinesterases

Volume: 6 Issue: 6

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

Affiliation:

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

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.

Cite this article as:

Jun Daniel, Paar Martin, Binder Jiri, Marek Jan, Pohanka Miroslav, Stodulka Petr and Kuca Kamil, Preparation and In Vitro Evaluation of Monoquaternary Inhibitors of Brain Cholinesterases, Letters in Organic Chemistry 2009; 6 (6) . https://dx.doi.org/10.2174/157017809789124876