The study of antiexudative action of S-alkylated 1,3,4-oxadiazole-3-thionе derivatives

Authors

  • Yu. L. Shepeta Vinnytsia National Pirogov Memorial Medical University, Ukraine,
  • A. V. Lozynskyi Danylo Halytsky Lviv National Medical University, Ukraine,
  • I. O. Nektiehaiev Danylo Halytsky Lviv National Medical University, Ukraine,
  • R. B. Lesyk Danylo Halytsky Lviv National Medical University, Ukraine,

DOI:

https://doi.org/10.14739/2409-2932.2019.3.184184

Keywords:

anti-inflammatory activity, carrageenan-induced rat paw inflammation, diclofenac, S-alkylated 1, 3, 4-oxadiazole-2-thiols

Abstract

Despite the popularity and efficiency of non-steroidal anti-inflammatory drugs and their widespread usage in clinical practice, this group of drugs is also characterized by numerous side effects, so obtaining of new safe NSAIDs is one of the priority tasks for modern pharmaceutical and medical chemistry.

Aim. Studying of the anti-inflammatory activity of S-alkylated 1,3,4-oxadiazole-2-thiol derivatives with diclofenac fragment in the molecules.

Materials and methods. The study of antiexudative activity of the compounds was carried out on the model of carrageenan-induced rat paw inflammation, quantitatively the effect was estimated by the index of inhibition of the inflammatory reaction.

Results. During the research, highly active S-alkylated derivatives of 1,3,4-oxadiazole-2-thiol with antiexudative activity in the range of 42.4–44.6 % were identified, which is commensurate with the effects of the reference drugs diclofenac sodium and ketorolac.

Conclusions. The obtained results indicate the presence of high antiexudative activity in a group of S-alkylated 1,3,4-oxadiazole-2-thiol derivatives, which actualizes the in-depth study of this class of heterocyclic compounds.

References

Shah, R. (2007). Dyspepsia and Helicobacter pylori. BMJ, 334, 41-43. doi: 10.1136/bmj.39014.468900.be

Anwar, A., John Anwar, I., & Delafontaine, P. (2015). Elevation of cardiovascular risk by non-steroidal anti-inflammatory drugs. Trends In Cardiovascular Medicine, 25(8), 726-735. doi: 10.1016/j.tcm.2015.03.006

Pirlamarla, P., & Bond, R. (2016). FDA labeling of NSAIDs: Review of nonsteroidal anti-inflammatory drugs in cardiovascular disease. Trends In Cardiovascular Medicine, 26(8), 675-680. doi: 10.1016/j.tcm.2016.04.011

Boschelli, D., Connor, D., Bornemeier, D., Dyer, R., Kennedy, J., & Kuipers, P. et al. (1993). 1,3,4-Oxadiazole, 1,3,4-thiadiazole, and 1,2,4-triazole analogs of the fenamates: in vitro inhibition of cyclooxygenase and 5-lipoxygenase activities. Journal Of Medicinal Chemistry, 36(13), 1802-1810. doi: 10.1021/jm00065a002

Shepeta, Yu. L., Leliukh, M. I., Roman, O. M., Zimenkovskyi, B.S., & Lesyk, R.B. (2015). Syntez s-alkilovanykh pokhidnykh 1,3,4-oksadiazol-2-tiolu z frahmentamy dyklofenaku ta ibuprofenu v molekulakh [Synthesis of s-alkylated 1,3,4-oxadiazole-3-thiol derivatives containing diclofenac and ibuprofen fragments in molecules]. Clinical pharmacy, pharmacotherapy & medical standartization, 3-4, 81-86. [in Ukrainian].

Stefanov, O. V. (Ed) (2001). Doklinichni doslidzhennia likarskykh zasobiv : metodychni rekomendatsii [Preclinical study of medicines: methodological recommendations]. Kiev: Avicenna.[in Ukrainian].

How to Cite

1.
Shepeta YL, Lozynskyi AV, Nektiehaiev IO, Lesyk RB. The study of antiexudative action of S-alkylated 1,3,4-oxadiazole-3-thionе derivatives. Current issues in pharmacy and medicine: science and practice [Internet]. 2019Nov.21 [cited 2024Jul.20];(3). Available from: http://pharmed.zsmu.edu.ua/article/view/184184

Issue

Section

Original research