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Novel fumarate derivatives; synthesis and investigation of acetylcholinesterase inhibitor properties

Year 2021, Volume: 8 Issue: 2, 544 - 551, 31.05.2021
https://doi.org/10.31202/ecjse.819956

Abstract

In this study, new fumarate compounds (I-IV) containing some natural phenols (eugenol, guaiacol, isoeugenol and vanillin) were synthesized and characterized. The single crystal X-ray diffraction technique was used to determine the crystal structures of all compounds. All compounds were evaluated as acetylcholinesterase (AChE) inhibitory, especially compound IV (IC50 =5.25±0.51 µg/mL), can be identified as a promising anti-acetylcholinesterase agent due to its good inhibitory effect, when compared with donepezil hydrochloride (IC50 =16.02±0.66 µg/mL) as used standard acetylcholinesterase inhibitory agent.

Project Number

FBA-2016-697

References

  • [1] Howes M.J.R., Houghton P.J., Pharmacol Biochem Be, 2003, 75, 513-27.
  • [2] Houghton P.J., Howes M.J., Lee C.C., Steventon G., J Ethnopharmacol, 2007, 110, 391-400.
  • [3] Wiener S.W., Hoffman R.S., J Intensive Care Med, 2004, 19, 22-37.
  • [4] Spatz S.M., J. Org. Chem., 1961, 26, 4158-61.
  • [5] Kantar G.K., Baltas N., Beris F.S., Sasmaz S., Curr. Enzyme Inhib., 2017, 13, 27-33.
  • [6] Şahin Z.S., Kantar G.K., Şaşmaz S., Büyükgüngör O., J Mol Struct, 2015, 1087, 104-12.
  • [7] Şahin Z.S., Kantar G.K., Şaşmaz S., Büyükgüngör O., J Mol Struct, 2016, 1103, 156-65.
  • [8] Mercury...............................................................................................................
  • [9] Spek A.L., Utrecht University, Utrecht, , 2005.
  • [10] Ellman G.L., Courtney K.D., Andres V., Featherstone R.M., Biochem Pharmacol, 1961, 7, 88-95.

Yeni fumarat türevlerinin sentezi ve asetilkolinesteraz inhibitörü etkilerinin araştırılması

Year 2021, Volume: 8 Issue: 2, 544 - 551, 31.05.2021
https://doi.org/10.31202/ecjse.819956

Abstract

Bu çalışmada, bazı doğal fenolleri (öjenol, guayakol, izoöjenol ve vanilin) içeren yeni fumarat bileşikleri (I-IV) sentezlenmiş ve karakterize edilmiştir. Tüm bileşiklerin kristal yapılarını belirlemek için tek kristal X-Işını kırınım tekniği kullanıldı. Tüm bileşikler asetilkolinesteraz (AChE) inhibitörü olabilecekmiş gibi değerlendirildi, özellikle bileşik IV (IC50 = 5.25 ± 0.51 µg / mL), donepezil hidroklorür (IC50 =16.02±0.66 µg/mL) ile karşılaştırıldığında, iyi inhibe edici etkisinden dolayı umut verici anti-asetilkolinesteraz ajanı olarak tanımlanabilir.

Supporting Institution

Recep Tayyip Erdoğan University

Project Number

FBA-2016-697

References

  • [1] Howes M.J.R., Houghton P.J., Pharmacol Biochem Be, 2003, 75, 513-27.
  • [2] Houghton P.J., Howes M.J., Lee C.C., Steventon G., J Ethnopharmacol, 2007, 110, 391-400.
  • [3] Wiener S.W., Hoffman R.S., J Intensive Care Med, 2004, 19, 22-37.
  • [4] Spatz S.M., J. Org. Chem., 1961, 26, 4158-61.
  • [5] Kantar G.K., Baltas N., Beris F.S., Sasmaz S., Curr. Enzyme Inhib., 2017, 13, 27-33.
  • [6] Şahin Z.S., Kantar G.K., Şaşmaz S., Büyükgüngör O., J Mol Struct, 2015, 1087, 104-12.
  • [7] Şahin Z.S., Kantar G.K., Şaşmaz S., Büyükgüngör O., J Mol Struct, 2016, 1103, 156-65.
  • [8] Mercury...............................................................................................................
  • [9] Spek A.L., Utrecht University, Utrecht, , 2005.
  • [10] Ellman G.L., Courtney K.D., Andres V., Featherstone R.M., Biochem Pharmacol, 1961, 7, 88-95.
There are 10 citations in total.

Details

Primary Language English
Subjects Engineering
Journal Section Makaleler
Authors

Günay Kaya Kantar 0000-0002-0259-0417

Project Number FBA-2016-697
Publication Date May 31, 2021
Submission Date February 22, 2021
Acceptance Date April 2, 2021
Published in Issue Year 2021 Volume: 8 Issue: 2

Cite

IEEE G. Kaya Kantar, “Novel fumarate derivatives; synthesis and investigation of acetylcholinesterase inhibitor properties”, El-Cezeri Journal of Science and Engineering, vol. 8, no. 2, pp. 544–551, 2021, doi: 10.31202/ecjse.819956.
Creative Commons License El-Cezeri is licensed to the public under a Creative Commons Attribution 4.0 license.
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