Synthesis and In Vitro Evaluation of N-(Bromobut-3-en-2-yl)-7-methoxy-1,2,3,4-tetrahydroacridin-9-amine as a Cholinesterase Inhibitor with Regard to Alzheimer's Disease Treatment
Abstract
:1. Introduction
2. Results and Discussion
3. Experimental
3.1. Chemistry
3.2. In vitro evaluation
3.3. Synthesis of N-(bromobut-3-en-2-yl)-7-methoxy-1,2,3,4-tetrahydroacridin-9-amine (1)
3.4. Molecular docking
4. Conclusion
Acknowledgements
References
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Sample Availability: Samples of the compounds THA, 7-MEOTA and 1 are available from authors. |
Compound | hAChE IC50 ± SD (µM) | hBChE IC50 ± SD (µM) | SI hBChE/hAChE |
---|---|---|---|
THA | 0.5 ± 0.1 | 0.02 ± 0.003 | 0.05 |
7-MEOTA | 15.0 ± 2.4 | 21.0 ± 3.4 | 1.4 |
1 | 89.1 ± 17.3 | 78.8 ± 12.8 | 0.88 |
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Korabecny, J.; Musilek, K.; Holas, O.; Nepovimova, E.; Jun, D.; Zemek, F.; Opletalova, V.; Patocka, J.; Dohnal, V.; Nachon, F.; Hroudova, J.; Fisar, Z.; Kuca, K. Synthesis and In Vitro Evaluation of N-(Bromobut-3-en-2-yl)-7-methoxy-1,2,3,4-tetrahydroacridin-9-amine as a Cholinesterase Inhibitor with Regard to Alzheimer's Disease Treatment. Molecules 2010, 15, 8804-8812. https://doi.org/10.3390/molecules15128804
Korabecny J, Musilek K, Holas O, Nepovimova E, Jun D, Zemek F, Opletalova V, Patocka J, Dohnal V, Nachon F, Hroudova J, Fisar Z, Kuca K. Synthesis and In Vitro Evaluation of N-(Bromobut-3-en-2-yl)-7-methoxy-1,2,3,4-tetrahydroacridin-9-amine as a Cholinesterase Inhibitor with Regard to Alzheimer's Disease Treatment. Molecules. 2010; 15(12):8804-8812. https://doi.org/10.3390/molecules15128804
Chicago/Turabian StyleKorabecny, Jan, Kamil Musilek, Ondrej Holas, Eugenie Nepovimova, Daniel Jun, Filip Zemek, Veronika Opletalova, Jiri Patocka, Vlastimil Dohnal, Florian Nachon, Jana Hroudova, Zdenek Fisar, and Kamil Kuca. 2010. "Synthesis and In Vitro Evaluation of N-(Bromobut-3-en-2-yl)-7-methoxy-1,2,3,4-tetrahydroacridin-9-amine as a Cholinesterase Inhibitor with Regard to Alzheimer's Disease Treatment" Molecules 15, no. 12: 8804-8812. https://doi.org/10.3390/molecules15128804