Araştırma Makalesi
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SYNTHESIS AND ANTIRADICAL ACTIVITY OF ALKYL DERIVATIVES OF 5-(5-METHYL-1H-PYRAZOL-3-YL)-4-PHENYL-4H1,2,4-TRIAZOLE-3-THIOL

Yıl 2020, , 211 - 219, 31.05.2020
https://doi.org/10.33483/jfpau.616116

Öz

Objective: The aim of the work was to develop effective methods for the synthesis of biologically active heterocyclic systems containing 1,2,4-triazole and pyrazole.
Material and Method: Chemical structures of synthesized compounds were characterized with elemental analysis, IR, 1H-NMR, LC-MS techniques. The antiradical activity was evaluated using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity assay.
Result and Discussion: Developed optimal methods of obtaining of alkylderivatives of 5-(5-methyl-1H-pyrazol-3-yl)-4-phenyl-4H-1,2,4-triazole-3-thiol. A number of synthesized compounds showed moderate antiradical activity.

Kaynakça

  • 1. Karrouchi, K., Radi, S., Ramli, Y., Taoufik, J., Mabkhot, Y., Al-aizari, F., Ansar, M. (2018). Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review. Molecules, 23, 134.
  • 2. Al-Ghamdi, H. M. (2019). Synthesis and antimicrobial activity of novel pyrazole derivatives. Oriental journal of chemistry, 35 (1), 391-398.
  • 3. Vijesh, A. M., Isloor, A. M., Shetty, P., Sundershan, S., Fun, H. K. (2013). New pyrazole derivatives containing 1,2,4-triazoles and benzoxazoles as potent antimicrobial and analgesic agents. European Journal of Medicinal Chemistry, 62, 410-415.
  • 4. Kharb, R., Sharma P. C., Bhandari, A., Yar, M. S. (2012). Synthesis, spectral characterization and anthelmintic evaluation of some novel imidazole bearing triazole derivatives / Der Pharmacia Lettre, 4 (2), 652-657.
  • 5. Hassan, G. S, Abdel Rahman D. E., Abdelmajeed E. A., Refaey R. H., Alaraby, S. M., Nissan, Y. M. (2019). New pyrazole derivatives: Synthesis, anti-inflammatory activity, cycloxygenase inhibition assay and evaluation of mPGES. Eurohean Journal of Medicinal Chemistry, 171, 332-342.
  • 6. Li, Y.-S., Tian, H., Zhao, D.-S., Hu, D.-K., Liu, X.-Y., Jin, H.-W., Cui, Z.-N. (2016). Synthesis and bioactivity of pyrazole and triazole derivatives as potential PDE4 inhibitors. Bioorganic & Medicinal Chemistry Letters, 26 (15), 3632-3635.
  • 7. Ashok, D., Kavitha, R., Gundu, S., Rao, V. H. (2017). Microwave-assisted synthesis of new pyrazole derivatives bearing 1,2,3-triazole scaffold as potential antimicrobial agents. Journal of the Serbian Chemical Society, 82 (4), 357-366.
  • 8. Hotsulia, A. S., Fedotov, S. O. (2019). Synthesis, structure and properties of N-R-2-(5-(5-methyl-1H-pyrazole-3-yl)-4-phenyl-4H-1,2,4-triazole-3-ylthio)acetamides / Current issues in pharmacy and medicine: science and practice, 12 (1), 4-9.
  • 9. Kazunin, M. S., Voskoboynik, O. Yu., Nosulenko, I. S., Berest, G. G., Sergeieva, T., Okovytyy, S., Karpenko, O. V., Priimenko, B. O., Kovalenko, S. I. (2018). Synthesis, Tautomerism, and Antiradical Activity of Novel Pteridinetrione Derivatives / Journal of Heterocyclic Chemistry, 55 (4), 1033-1041.

5-(5-METİL-1H-PİRAZOL-3-İL)-4-FENİL-4H-1,2,4-TRİAZOL-3-TİYOL ALKİL TÜREVLERİNİN SENTEZ VE ANTİRADİKAL AKTİVİTELERİ

Yıl 2020, , 211 - 219, 31.05.2020
https://doi.org/10.33483/jfpau.616116

Öz

Amaç: Çalışmanın amacı biyolojik olarak aktif 1,2,4-triazol ve pirazol içeren heterosiklik sistemlerin sentezi için etkili yöntemler geliştirmektir.
Gereç ve Yöntem: Sentezlenen bileşiklerin kimyasal yapıları elemantal analiz, IR, 1H-NMR, LC-MS teknikleri ile karakterize edildi. Antiradikal aktivite 2,2-difenil-1-pikrilhidrazil (DPPH) radikal süpürücü aktivite deneyi kullanılarak değerlendirildi.
Sonuç ve Tartışma: 5-(5-metil-1H-pirazol-3-il)-4-fenil-4H-1,2,4-triazol-3-tiyol alkil türevlerinin elde edilmesi için optimum yöntemler geliştirildi. Bir dizi sentezlenmiş bileşik, orta derecede antiradikal aktivite göstermiştir.

Kaynakça

  • 1. Karrouchi, K., Radi, S., Ramli, Y., Taoufik, J., Mabkhot, Y., Al-aizari, F., Ansar, M. (2018). Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review. Molecules, 23, 134.
  • 2. Al-Ghamdi, H. M. (2019). Synthesis and antimicrobial activity of novel pyrazole derivatives. Oriental journal of chemistry, 35 (1), 391-398.
  • 3. Vijesh, A. M., Isloor, A. M., Shetty, P., Sundershan, S., Fun, H. K. (2013). New pyrazole derivatives containing 1,2,4-triazoles and benzoxazoles as potent antimicrobial and analgesic agents. European Journal of Medicinal Chemistry, 62, 410-415.
  • 4. Kharb, R., Sharma P. C., Bhandari, A., Yar, M. S. (2012). Synthesis, spectral characterization and anthelmintic evaluation of some novel imidazole bearing triazole derivatives / Der Pharmacia Lettre, 4 (2), 652-657.
  • 5. Hassan, G. S, Abdel Rahman D. E., Abdelmajeed E. A., Refaey R. H., Alaraby, S. M., Nissan, Y. M. (2019). New pyrazole derivatives: Synthesis, anti-inflammatory activity, cycloxygenase inhibition assay and evaluation of mPGES. Eurohean Journal of Medicinal Chemistry, 171, 332-342.
  • 6. Li, Y.-S., Tian, H., Zhao, D.-S., Hu, D.-K., Liu, X.-Y., Jin, H.-W., Cui, Z.-N. (2016). Synthesis and bioactivity of pyrazole and triazole derivatives as potential PDE4 inhibitors. Bioorganic & Medicinal Chemistry Letters, 26 (15), 3632-3635.
  • 7. Ashok, D., Kavitha, R., Gundu, S., Rao, V. H. (2017). Microwave-assisted synthesis of new pyrazole derivatives bearing 1,2,3-triazole scaffold as potential antimicrobial agents. Journal of the Serbian Chemical Society, 82 (4), 357-366.
  • 8. Hotsulia, A. S., Fedotov, S. O. (2019). Synthesis, structure and properties of N-R-2-(5-(5-methyl-1H-pyrazole-3-yl)-4-phenyl-4H-1,2,4-triazole-3-ylthio)acetamides / Current issues in pharmacy and medicine: science and practice, 12 (1), 4-9.
  • 9. Kazunin, M. S., Voskoboynik, O. Yu., Nosulenko, I. S., Berest, G. G., Sergeieva, T., Okovytyy, S., Karpenko, O. V., Priimenko, B. O., Kovalenko, S. I. (2018). Synthesis, Tautomerism, and Antiradical Activity of Novel Pteridinetrione Derivatives / Journal of Heterocyclic Chemistry, 55 (4), 1033-1041.
Toplam 9 adet kaynakça vardır.

Ayrıntılar

Birincil Dil İngilizce
Konular Eczacılık ve İlaç Bilimleri
Bölüm Araştırma Makalesi
Yazarlar

Andrey Gotsulya 0000-0001-9696-221X

Yayımlanma Tarihi 31 Mayıs 2020
Gönderilme Tarihi 6 Eylül 2019
Kabul Tarihi 8 Mart 2020
Yayımlandığı Sayı Yıl 2020

Kaynak Göster

APA Gotsulya, A. (2020). SYNTHESIS AND ANTIRADICAL ACTIVITY OF ALKYL DERIVATIVES OF 5-(5-METHYL-1H-PYRAZOL-3-YL)-4-PHENYL-4H1,2,4-TRIAZOLE-3-THIOL. Journal of Faculty of Pharmacy of Ankara University, 44(2), 211-219. https://doi.org/10.33483/jfpau.616116
AMA Gotsulya A. SYNTHESIS AND ANTIRADICAL ACTIVITY OF ALKYL DERIVATIVES OF 5-(5-METHYL-1H-PYRAZOL-3-YL)-4-PHENYL-4H1,2,4-TRIAZOLE-3-THIOL. Ankara Ecz. Fak. Derg. Mayıs 2020;44(2):211-219. doi:10.33483/jfpau.616116
Chicago Gotsulya, Andrey. “SYNTHESIS AND ANTIRADICAL ACTIVITY OF ALKYL DERIVATIVES OF 5-(5-METHYL-1H-PYRAZOL-3-YL)-4-PHENYL-4H1,2,4-TRIAZOLE-3-THIOL”. Journal of Faculty of Pharmacy of Ankara University 44, sy. 2 (Mayıs 2020): 211-19. https://doi.org/10.33483/jfpau.616116.
EndNote Gotsulya A (01 Mayıs 2020) SYNTHESIS AND ANTIRADICAL ACTIVITY OF ALKYL DERIVATIVES OF 5-(5-METHYL-1H-PYRAZOL-3-YL)-4-PHENYL-4H1,2,4-TRIAZOLE-3-THIOL. Journal of Faculty of Pharmacy of Ankara University 44 2 211–219.
IEEE A. Gotsulya, “SYNTHESIS AND ANTIRADICAL ACTIVITY OF ALKYL DERIVATIVES OF 5-(5-METHYL-1H-PYRAZOL-3-YL)-4-PHENYL-4H1,2,4-TRIAZOLE-3-THIOL”, Ankara Ecz. Fak. Derg., c. 44, sy. 2, ss. 211–219, 2020, doi: 10.33483/jfpau.616116.
ISNAD Gotsulya, Andrey. “SYNTHESIS AND ANTIRADICAL ACTIVITY OF ALKYL DERIVATIVES OF 5-(5-METHYL-1H-PYRAZOL-3-YL)-4-PHENYL-4H1,2,4-TRIAZOLE-3-THIOL”. Journal of Faculty of Pharmacy of Ankara University 44/2 (Mayıs 2020), 211-219. https://doi.org/10.33483/jfpau.616116.
JAMA Gotsulya A. SYNTHESIS AND ANTIRADICAL ACTIVITY OF ALKYL DERIVATIVES OF 5-(5-METHYL-1H-PYRAZOL-3-YL)-4-PHENYL-4H1,2,4-TRIAZOLE-3-THIOL. Ankara Ecz. Fak. Derg. 2020;44:211–219.
MLA Gotsulya, Andrey. “SYNTHESIS AND ANTIRADICAL ACTIVITY OF ALKYL DERIVATIVES OF 5-(5-METHYL-1H-PYRAZOL-3-YL)-4-PHENYL-4H1,2,4-TRIAZOLE-3-THIOL”. Journal of Faculty of Pharmacy of Ankara University, c. 44, sy. 2, 2020, ss. 211-9, doi:10.33483/jfpau.616116.
Vancouver Gotsulya A. SYNTHESIS AND ANTIRADICAL ACTIVITY OF ALKYL DERIVATIVES OF 5-(5-METHYL-1H-PYRAZOL-3-YL)-4-PHENYL-4H1,2,4-TRIAZOLE-3-THIOL. Ankara Ecz. Fak. Derg. 2020;44(2):211-9.

Kapsam ve Amaç

Ankara Üniversitesi Eczacılık Fakültesi Dergisi, açık erişim, hakemli bir dergi olup Türkçe veya İngilizce olarak farmasötik bilimler alanındaki önemli gelişmeleri içeren orijinal araştırmalar, derlemeler ve kısa bildiriler için uluslararası bir yayım ortamıdır. Bilimsel toplantılarda sunulan bildiriler supleman özel sayısı olarak dergide yayımlanabilir. Ayrıca, tüm farmasötik alandaki gelecek ve önceki ulusal ve uluslararası bilimsel toplantılar ile sosyal aktiviteleri içerir.