The analgesic activity research for the derivatives of 4-R-3-(morpholinomethylene)-1,2,4-triazole-5-thioles

  • E. V. Kapelyanovich Zaporizhzhіa State Medical University
  • R. O. Shcherbyna Zaporizhzhіa State Medical University
  • E. S. Pruglo Zaporizhzhіa State Medical University
  • O. I. Panasenko Zaporizhzhіa State Medical University
  • Ye. H. Knysh Zaporizhzhіa State Medical University
Keywords: derivatives of 1,2,4-triazole, analgesic activity, «structure–action»

Abstract

Pain is a protective reaction of the organism, which is the first sign of illness or signal of danger. Existing drugs for pain reducing exhibits a series of side effects. However, with an analgesic effect, most of these preparations displays lot of side effects. Thus, the searching for new highly effective and safe drug with pronounced analgesic activity is an actual problem of modern medicine and pharmacy.

The purpose of our studies was to investigate the analgesic properties of some derivatives of 4-R-3-(morpholinomethylene)-1,2,4-triazole-5-thioles and detection of some regularities according to pharmacological activity and the chemical structure of synthesized compounds.

For studying the analgesic effect of new derivatives of 1,2,4-triazole, and determine the effect of the central component in the nociceptive system the model of thermal limbs stimulation («hot plate») was used.

The study has found of that most from tested compounds under the experimental conditions reduced the pain threshold in laboratory animals. However, the replacement of methyl substituent at N1 atom of nitrogen in molecule 3-(morpholinomethylene)-4-methyl-1,2,4-triazole-5-thiol (PKR-125) for phenyl substituent (PKR-123) leads to a slight analgesic activity. It has been established, that the appearance of carboxylic group in the molecule reduces the analgesic effect of some synthesized compounds.

References

1. Vertkin A. L., Vovk E. I., Naumov A. V., Goruleva E. I. Nekotorye voprosy differencirovannogo naznacheniya sovremennyh lekarstvennyh preparatov dlya terapii ostroj boli // Medicina neotlozhnyh sostoyanij. – 2006. – № 1 (2). – S. 91–98.
2. Shevaga V. M. Zahvoryuvannya nervovoyi sistemi. – Lviv: Svit, 2004. – 520 s.
3. Nasonov E. L. Nesteroidnye protivovospalitelnye preparaty v revmatologii // Lechashij vrach. – 2006. – № 2. – S. 50–53.
4. Finkelshtejn L. O. Boleutolyayushie sredstva / Enciklopedicheskij slovar Brokgauza i Efrona: v 86 tomah (82 t. i 4 dop.). – SPb. – S. 1890-1907.
5. Habriev R. U. Rukovodstvo po eksperimentalnomu (doklinicheskomu) izucheniyu novyh farmakologicheskih veshestv. – M.: Medicina, 2005. – 832 s.
6. Viktorov A. P., Shevchenko T. L., Kashuba A. V. Analgetiki-antipiretiki: bezopasnost pri medicinskom primenenii // Medicinskie aspekty zdorovya zhenshiny. – 2010. – № 9–10 (38). – S. 39–54.
7. Rebrova O. Yu. Statisticheskij analiz medicinskih dannyh. Primenenie paketa prikladnyh programm STATISTICA. – M.: Media Sfera, 2006. – 312 s.
8. Lapach S. N., Chubenko A. B., Babich P. N. Statisticheskie metody v mediko-biologicheskih issledovaniyah s ispolzovaniem Excel. – K.: Morion, 2001. – 408 s.
Published
2019-02-12
How to Cite
Kapelyanovich, E. V., Shcherbyna, R. O., Pruglo, E. S., Panasenko, O. I., & Knysh, Y. H. (2019). The analgesic activity research for the derivatives of 4-R-3-(morpholinomethylene)-1,2,4-triazole-5-thioles. Farmatsevtychnyi Zhurnal, (6), 100-104. Retrieved from https://pharmj.org.ua/index.php/journal/article/view/280
Section
General and Clinical Pharmacology