The study of antiexudative action of S-alkylated 1,3,4-oxadiazole-3-thionе derivatives
Keywords:anti-inflammatory activity, carrageenan-induced rat paw inflammation, diclofenac, S-alkylated 1, 3, 4-oxadiazole-2-thiols
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.
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
Authors who publish with this journal agree to the following terms:
- Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution License that allows others to share the work with an acknowledgement of the work's authorship and initial publication in this journal.
- Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgement of its initial publication in this journal.
- Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (See The Effect of Open Access)