Abstract
New dual binding site acetylcholinesterase (AChE) inhibitors have been designed and synthesized as a new drug candidate for the treatment of Alzheimer’s disease (AD) through the binding to both catalytic and peripheral sites of the enzyme. Therefore, a series of thienopyridine analogs of tacrine were synthesized and investigated for their ability to inhibit the activity of AChE in comparison with tacrine. All the compounds were found to inhibit AChE activity, especially compounds 7b and 11a, which were found to be more potent than tacrine.
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Acknowledgments
The authors are very grateful to the staff members of the Department of Pharmacology, Faculty of Pharmacy, Cairo University, for carrying out the pharmacological screening of the newly synthesized compounds.
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Badran, M.M., Hakeem, M.A., Abuel-Maaty, S.M. et al. Design and synthesis of thienopyridines as novel templates for acetylcholinesterase inhibitors. Med Chem Res 22, 4087–4095 (2013). https://doi.org/10.1007/s00044-012-0403-5
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DOI: https://doi.org/10.1007/s00044-012-0403-5