Comparison of Novel Tacrine and 7-MEOTA Derivatives with Aromatic and Alicyclic Residues: Synthesis, Biological Evaluation and Docking Studies

Title:Comparison of Novel Tacrine and 7-MEOTA Derivatives with Aromatic and Alicyclic Residues: Synthesis, Biological Evaluation and Docking Studies

Volume: 10 Issue: 4

Author(s): Jan Korabecny, Ladislav Janovec, Kamil Musilek, Filip Zemek, Anna Horova, Eugenie Nepovimova, Rafael Dolezal, Veronika Opletalova, Jana Hroudova, Zdenek Fisar, Young-Sik Jung and Kamil Kuca

Affiliation:

Keywords: 7-methoxytacrine, acetylcholinesterase, Alzheimer`s disease, butyrylcholinesterase, inhibition selectivity, molecular modelling.

Abstract: Cholinesterase inhibitors play an essential role in the treatment of Alzheimer’s disease. Since their first introduction over a decade ago, they are an indispensable part of Alzheimer’s disease therapy and remain at the forefront of scientific interest worldwide. In this manuscript new analogs of THA and 7-MEOTA were designed, synthesized, and evaluated for their inhibitory activity against both acetylcholinesterase and butyrylcholinesterase. Cholinergic properties were investigated and quantified with respect to their side chain residues (aromatic or alicyclic). All synthesized compounds proved to have potent inhibitory activity at micromolar range. Moreover, compound 4 demonstrated promising efficacy and appears to be an ideal candidate for further testing.

Cite this article as:

Korabecny Jan, Janovec Ladislav, Musilek Kamil, Zemek Filip, Horova Anna, Nepovimova Eugenie, Dolezal Rafael, Opletalova Veronika, Hroudova Jana, Fisar Zdenek, Jung Young-Sik and Kuca Kamil, Comparison of Novel Tacrine and 7-MEOTA Derivatives with Aromatic and Alicyclic Residues: Synthesis, Biological Evaluation and Docking Studies, Letters in Organic Chemistry 2013; 10 (4) . https://dx.doi.org/10.2174/1570178611310040011