Design, One-Pot Synthesis, and Evaluation of 7H-Thiazolo[3,2-b]-1,2,4-Triazin-7-One Derivatives as Dual Binding Site Acetylcholinesterase Inhibitors

Si Jie Liu; Lan Xiang Shi; Jing Yu He; Li Bo Cui

doi:10.4028/www.scientific.net/AMR.884-885.607

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HomeAdvanced Materials ResearchAdvanced Materials Research Vols. 884-885Design, One-Pot Synthesis, and Evaluation of...

Design, One-Pot Synthesis, and Evaluation of 7H-Thiazolo[3,2-b]-1,2,4-Triazin-7-One Derivatives as Dual Binding Site Acetylcholinesterase Inhibitors

Abstract:

In order to study the the structure-AChE inhibitory activity relationships of 7H-thiazolo [3,2-b]-1,2,4-triazin-7-one derivatives, the 7H-thiazolo[3,2-b]-1,2,4-triazin-7-ones were designed by molecular docking, and readily prepared via a one-pot reaction in N-methyl pyrrolidone hydrosulfate ([Hnmp]HSO₄) lonic liquid. The study of AChE inhibitory activity was carried out using the Ellman colorimetric assay with huperzine-A as the positive control drug. Most of the target compounds exhibited more than 50% inhibition at 10μM.

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Periodical:

Advanced Materials Research (Volumes 884-885)

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607-610

DOI:

https://doi.org/10.4028/www.scientific.net/AMR.884-885.607

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Online since:

January 2014

Authors:

Si Jie Liu*, Lan Xiang Shi, Jing Yu He, Li Bo Cui

Keywords:

7H-thiazolo[3,2-b]-1,2,4-Triazin-7-One Derivatives, Acetylcholinesterase Inhibitor, Biological Activity, Docking, One-Pot Synthesis

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References

[1] A. Skrzypek, J. Matysiak, A. Niewiadomy, M. Bajda, Synthesis and biological evaluation of 1, 3, 4-thiadiazole analogues as novel AChE and BuChE inhibitors, Eur. J. Med. Chem. 62 (2013) 311-319.

DOI: 10.1016/j.ejmech.2012.12.060

Google Scholar

[2] G. Pepeu, M. G. Giovannini, Cholinesterase inhibitors and beyond, Curr. Alzheimer. Res. 6 (2009) 86-96.

DOI: 10.2174/156720509787602861

Google Scholar

[3] S. J. Liu, L. Yang, Z. Jin, E. Huang, D. Wan, H. Lin, C. Hu, Design, synthesis, and biological evaluation of 7H-thiazolo[3, 2-b]-1, 2, 4-triazin-7-one derivatives as novel acetylcholinesterase inhibitors, ARKIVOC 10 (2009) 333-348.

DOI: 10.3998/ark.5550190.0010.a30

Google Scholar

[4] S. J. Liu, L. Yang, X. Liu, D. Wan, H. Lin, C. Hu, Design, Synthesis, and Biological Evaluation of 7H-thiazolo[3, 2-b]-1, 2, 4-triazin-7-one Derivatives as Acetylcholinesterase Inhibitors, Lett. Drug. Des. Discov. 7 (2010) 5-8.

DOI: 10.2174/157018010789869343

Google Scholar

[5] G. L. Ellman, K. D. Courtney, V. J. Andres, R. M. A. Featherstone, A new and rapid colorimetric determination of acetylcholinesterase activity, Biochem. Pharmacol. 7 (1961) 88-90.

DOI: 10.1016/0006-2952(61)90145-9

Google Scholar

[6] G. Kryger, M. Harel, K. Giles, L. Toker, B. Velan, A. Lazar, C. Kronman, J. L. Sussman, Structures of recombinant native and E202Q mutant human acetylcholinesterase complexed with the snake-venom toxin fasciculin-II, Acta Crystallogr. Sect.D. 56(2000).

DOI: 10.1107/s0907444900010659

Google Scholar