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Issue 5, 2011
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Tacrine-mefenamic acid hybrids for inhibition of acetylcholinesterase

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Alzheimer's disease (AD) is a complex syndrome characterized by the degeneration of the brain and central nervous system that may be caused by an assortment of genetic and environmental factors. Consequently, a conjunctive approach targeting multiple affecters of AD could lead to improved drug candidates for the treatment of AD. A convergent chemical synthetic approach yielded a series of tacrine-mefenamic acid hybrids that were evaluated for their ability to inhibit acetylcholinesterase (AChE). A majority of the compounds tested showed low nanomolar IC50 values, an improvement over the parent compound, tacrine, suggesting that they could be effective in increasing cholinergic function. Additionally, an assay to evaluate the compounds upon exposure to reactive oxygen species was performed, the results of which may suggest a role for the mefenamic acid moiety in the inhibition of AChE. Molecular modeling studies were performed to rationalize the experimental results.

Graphical abstract: Tacrine-mefenamic acid hybrids for inhibition of acetylcholinesterase

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The article was received on 10 Dec 2010, accepted on 15 Feb 2011 and first published on 09 Mar 2011

Article type: Concise Article
DOI: 10.1039/C0MD00256A
Med. Chem. Commun., 2011,2, 406-412

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    Tacrine-mefenamic acid hybrids for inhibition of acetylcholinesterase

    J. J. Bornstein, T. J. Eckroat, J. L. Houghton, C. K. Jones, K. D. Green and S. Garneau-Tsodikova, Med. Chem. Commun., 2011, 2, 406
    DOI: 10.1039/C0MD00256A

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