Journals / International Journal of Chemistry and Technology / 2024 / Volume: 8 Issue: 2

The enzyme kinetic studies, DNA protection and antioxidant activities of furan/ thiophene-2-carboxamide derivatives

Şükriye Çakmak(SİNOP ÜNİVERSİTESİ)0000-0002-2221-0098
Semiha Yenigün(ONDOKUZ MAYIS ÜNİVERSİTESİ)0000-0002-1979-5427
Tevfik Ozen(ONDOKUZ MAYIS ÜNİVERSİTESİ)0000-0003-0133-5630
Pages
—
Publication Date
2024-12-31
🏛️Bibliographic metadata and full text access for this article are provided via DergiPark.
DergiPark Record ↗
✨

AI Summary & Key Takeaways

AI Insight
⚡ TL;DR(Too Long; Didn't Read)

The findings suggest that thiophene/furan carboxy amide-containing CPD1 and CPD3 might be exploited as potential structures for evaluating pharmaceuticals with greater potency.

📌 3 Key Takeaways

🎯
Objective & Hypothesis:Three furan and/or thiophene-2-carboxamide compounds, namely N-(furan-2-ylmethyl)thiophene-2-carboxamide (1), N-(furan-2-carbonyl)furan-2-carboxamide (2), and N-(Thiophene-2-ylmethyl)furan-2-carboxamide (3) were investigated the enzyme kinetic studies by urease, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE).
📊
Key Findings & Data:The inhibition constant (Ki) of Compound (CPD)3 by AChE was determined as 0.10 mM, and the Ki value by BChE was determined as 0.07 mM.
💡
Conclusion & Impact:The findings suggest that thiophene/furan carboxy amide-containing CPD1 and CPD3 might be exploited as potential structures for evaluating pharmaceuticals with greater potency.
🔬Design:Research Article
📍Scope:Comprehensive Sample
⚙️Variables:Furan/thiophene-2-carboxamide · acetylcholinesterase · butyrylcholinesterase

Abstract

Three furan and/or thiophene-2-carboxamide compounds, namely N-(furan-2-ylmethyl)thiophene-2-carboxamide (1), N-(furan-2-carbonyl)furan-2-carboxamide (2), and N-(Thiophene-2-ylmethyl)furan-2-carboxamide (3) were investigated the enzyme kinetic studies by urease, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE). The inhibition constant (Ki) of Compound (CPD)3 by AChE was determined as 0.10 mM, and the Ki value by BChE was determined as 0.07 mM. In comparison, the Ki value of CPD1 by urease was determined as 0.10 mM. These CPDs were examined for antioxidant activity by the DPPH˙ scavenging method. CPD3 exhibited 98.93% DPPH scavenging activity compared to ascorbic acid, the positive control group. Furthermore, the DNA-protective activities of the compounds were investigated, and the DNA protection activity of CPD1 was observed to be 78%. The findings suggest that thiophene/furan carboxy amide-containing CPD1 and CPD3 might be exploited as potential structures for evaluating pharmaceuticals with greater potency.

🔖

Cite This Article

Çakmak, Ş., Yenigün, S., Ozen, T. (2024). The enzyme kinetic studies, DNA protection and antioxidant activities of furan/ thiophene-2-carboxamide derivatives. International Journal of Chemistry and Technology, Volume: 8 Issue: 2. https://doi.org/10.32571/ijct.1405155

📄 Full Text PDF Viewer

📄

PDF görüntüleyici hazırlanıyor...

References (38)

  1. Volodina, Y. L.; Tikhomirov, A. S.; Dezhenkova, L. G.; Ramonova, A. A.; Kononova, A. V.; Andreeva, D. V.; Kaluzhny, D. N.; Schols, D.; Moisenovich, M. M.; Shchekotikhin, A. E., 2021, Eur J Med Chem, 221, 113521.
  2. Owa, T.; Nagasu, T., 2000, Expert Opin Ther Pat, 10 (11), 1725-1740.
  3. Nan, X.; Wang, Q.-X.; Xing, S.-J.; Liang, Z.-G., 2023, J Enzym Inhib Med Ch, 38 (1), 2247183.
  4. Mali, S. N.; Anand, A.; Zaki, M. E.; Al-Hussain, S. A.; Jawarkar, R. D.; Pandey, A.; Kuznetsov, A., 2023, Molecules, 28 (6), 2801.
  5. Huang, E.; Zhang, L.; Xiao, C.; Meng, G.; Zhang, B.; Hu, J.; Wan, D. C.-C.; Meng, Q.; Jin, Z.; Hu, C., 2019, Chinese Chem Lett, 30 (12), 2157-2159.
  6. Desantis, J.; Nannetti, G.; Massari, S.; Barreca, M. L.; Manfroni, G.; Cecchetti, V.; Palù, G.; Goracci, L.; Loregian, A.; Tabarrini, O., 2017, Eur J Med Chem, 138, 128-139.
  7. Rollet-Labelle, E.; Grange, M.-J.; Elbim, C.; Marquetty, C.; Gougerot-Pocidalo, M.-A.; Pasquier, C., 1998, Free Radical Bio Med, 24 (4), 563-572.
  8. Singh, P.; Vishwakarma, S. P.; Singh, R. L., 2014, J Sci Food Agr, 94 (12), 2497-2504.
  9. Moskovitz, J.; Yim, M. B.; Chock, P. B., 2002, Arch Biochem Biophys, 397 (2), 354-359.
  10. Sevgi, K.; Tepe, B.; Sarikurkcu, C., 2015, Food Chem Toxicol, 77, 12-21.
  11. Cakmak, S.; Yenigun, S.; Ozen, T., 2023, J Iran Chem Soc, 20 (10), 2543-2553.
  12. Zhang, L.; Mulrooney, S. B.; Leung, A. F.; Zeng, Y.; Ko, B. B.; Hausinger, R. P.; Sun, H., 2006, Biometals, 19 (5), 503-511.
  13. Ellman, G. L.; Courtney, K. D.; Andres Jr, V.; Featherstone, R. M., 1961, Biochem Pharmacol, 7 (2), 88-95.
  14. Wu, Z.; Shen, L.; Han, Q.; Lu, J.; Tang, H.; Xu, X.; Xu, H.; Huang, F.; Xie, J.; He, Z., 2017, Food Biophys, 12 (1), 78-87.
  15. Blois, M. S., 1958, Nature, 181 (4617), 1199-1200.
  16. Baiseitova, A.; Jenis, J.; Kim, J. Y.; Li, Z. P.; Park, K. H., 2021, Nat Prod Res, 35 (5), 880-883.
  17. Başar, Y.; Demirtaş, İ.; Yenigün, S.; İpek, Y.; Özen, T.; Behçet, L., 2024, J Biomol Struct Dyn, 1-14.
  18. Basar, Y.; Yenigun, S.; Gul, F.; Ozen, T.; Demirtas, I. A., M. Hakkı; Temel, S., 2024, Int J Chem Techno, 8 (1), 62-71.
  19. Gökçimen, S. Ş.; İpek, Y.; Behçet, L.; Demirtaş, İ.; Özen, T., 2024, J Biomol Struct Dyn, Published online: 12 Jan 2024, 1-18.
  20. Başar, Y.; Yenigün, S.; İpek, Y.; Behçet, L.; Gül, F.; Özen, T.; Demirtaş, İ., 2023, J Biomol Struct Dyn, Published online.
  21. Yenigün, S.; Başar, Y.; İpek, Y.; Behçet, L.; Özen, T.; Demirtaş, İ., 2024, J Biomol Struct Dyn, 42 (11), 5799-5816.
  22. Afshari, M.; Rahimmalek, M.; Miroliaei, M.; Sabzalian, M. R.; Sadeghi, M.; Matkowski, A.; Szumny, A., 2024, Ind Crop Prod, 208, 117859.
  23. Yenigun, S.; Basar, Y.; Gül, F.; Ipek, Y.; Gok, M.; Behcet, L.; Ozen, T.; Demirtas, I., 2024, ChemistrySelect, 9 (18), e202400919.
  24. Yenigun, S.; Basar, Y.; Ipek, Y.; Gok, M.; Behcet, L.; Ozen, T.; Demirtas, I., 2024, Process Biochem, 143, 234-247.
  25. Yenigün, S.; Ozen, T.; Başar, Y.; Ipek, Y.; Gök, M.; Behçet, L.; Demirtaş, İ., 2024, Curr Persp Med Aromatic Plants, 7 (1), 1-11.
  26. Kareem, H. S.; Nordin, N.; Heidelberg, T.; Abdul-Aziz, A.; Ariffin, A., 2016, Molecules, 21 (2), 224.
  27. Takahashi, O.; Kirikoshi, R., 2014, Comput Sci Disc, 7 (1), 015005.
  28. Iqbal, A.; Khan, Z. A.; Shahzad, S. A.; Usman, M.; Khan, S. A.; Fauq, A. H.; Bari, A.; Sajid, M. A., 2018, Turkish J Chem, 42 (6), 1518-1533.
  29. Valko, M.; Leibfritz, D.; Moncol, J.; Cronin, M. T.; Mazur, M.; Telser, J., 2007, The Int J Biochem Cell Bio, 39 (1), 44-84.
  30. Azqueta, A.; Collins, A., 2016, Nutrients, 8 (12), 785.
  31. Bekhouche, K.; Ozen, T.; Boussaha, S.; Koldas, S.; Yenigun, S.; Lassed, S.; Demirtas, I.; Benayache, F.; Benayache, S.; Zama, D., 2018, Bangladesh J Pharmacol, 13 (1).
  32. Mondal, N. K.; Sorensen, E.; Hiivala, N.; Feller, E.; Griffith, B.; Wu, Z. J., 2013, Int J Med Sci, 10 (7), 883.
  33. Ozen, T.; Yenigun, S.; Toka, M., 2022, Int J Chem Techno, 6 (1), 21-32.
  34. Tuteja, N.; Singh, M. B.; Misra, M. K.; Bhalla, P. L.; Tuteja, R., 2001, Crit Rev Biochem Mol, 36 (4), 337-397.
  35. Valko, M.; Izakovic, M.; Mazur, M.; Rhodes, C. J.; Telser, J., 2004, Mol Cell Biochem, 266 (1-2), 37-56.
  36. Yenigun, S.; Ipek, Y.; Marah, S.; Demirtas, I.; Ozen, T., 2024, J Biomol Struct Dyn, 42 (2), 848-862.
  37. De Almeida, S. M. V.; Lafayette, E. A.; Da Silva, L. P. B. G.; Amorim, C. A. d. C.; De Oliveira, T. B.; Ruiz, A. L. T. G.; De Carvalho, J. E.; De Moura, R. O.; Beltrão, E. I. C.; De Lima, M. D. C. A., 2015, Int J Mol Sci, 16 (6), 13023-13042.
  38. Basar, Y.; Yenigun, S.; Gul, F.; Ozen, T.; Demirtas, I. A., M. Hakkı; Temel, S., 2024, Int J Chem Techno, 8 (1), 62-71.