The research of acute toxicity of 4-amino-5-(4-(tert-butyl)phenyl)-4H-1,2,4-triazoles-3-thiol derivatives

Authors

  • I. I. Аksyonova-Seliuk Zaporizhzhia State Medical University,
  • Ye. S. Pruglo Zaporizhzhia State Medical University,
  • O. I. Panasenko Zaporizhzhia State Medical University,
  • Ye. G. Knysh Zaporizhzhia State Medical University,

DOI:

https://doi.org/10.14739/2409-2932.2017.2.103771

Keywords:

1, 2, 4-triazoles, acute toxicity, lethal dose

Abstract

Introduction. The process of new drugs creating includes a plurality of stages, which allow their application in medical practice in the future. These studies are a guarantee of the effectiveness and safety of the test compounds. One of the most important stages of preclinical research is the research of acute toxicity. The data of this experiment gives an estimate of toxic effect of new compounds on the organism of experimental animals that allows to judge about expediency of application of these substances in diseases therapy.

The aim of toxicological researches of 4-amino-5-(4-(tert-butyl)phenyl)-4H-1,2,4-triazoles-3-thiol’s derivatives was to establish their damaging effect on the organism of experimental rats and identify possible influence of chemical structure on acute toxicity of the compounds.

Methods and results. The tabular rapid-method by V. B. Prozorovsky was chosen. It’s based on the test-compounds dosing according to a logarithmic scale. Two animals were used for the study of one dose of the compound. Animals were pre-weighed and labeled, also an assessment of their external condition was carried out. According to the results of the study, it was found that the compounds belong to the IV class of toxicity according to the classification of K. K. Sidorov.

Conclusion. Assessment of toxicity of 31 new compounds, namely derivatives of 4-amino-5-(4-(tert-butyl)phenyl)-4H-1,2,4-triazoles-3-thiol was carried out. The experiments allowed to establish LD50 of test compounds. The most toxic and the least toxic compounds were found. The results of research make it possible to determine some "structure-action" dependence.

References

Nakaz Ukrainy «Pro zatverdzhennia Poriadku provedennia doklinichnoho vyvchennia likarskykh zasobiv ta ekspertyzy materialiv doklinichnoho vyvchennia likarskykh zasobiv» vid 14.12.2009 r. №944 [Order of Ukraine On approval of the clinical trial and preclinical expertise of medicines from December 14, 2009, №944] Retrieved from http://zakon0.rada.gov.ua/laws/show/z0053-10. [in Ukrainian].

Mironov, A. N., Bunatyan, N. D., et al. (2012) Rukovodstvo po provedeniyu doklinicheskikh issledovanij lekarstvennykh sredstv [A guide to preclinical drug research]. Moscow: Grif i K. [in Russian].

Prozorovskii, V. B. (2007) Statisticheskaya obrabotka rezul'tatov farmakologicheskikh issledovanij [Statistic processing of data of pharmacological investigations]. Psikhofarmakologiya i biologicheskaya narkologiya, 7(3–4), 2090–2120. [in Russian].

Prozorovskij, V. B. (1998) Tablichnyj e´kspress-metod opredeleniya srednikh e´ffektivnykh mer vozdejstviya na biologicheskiye ob"yekty [Tabular express method for determining the average effective measures of action on biological objects]. Toksikologicheskij vestnik, 1, 28–32. [in Russian].

Sidorov, K. K. (1973) O klassifikacii toksichnosti yadov pri parenteral'nykh sposobakh vvedeniya [On the classification of the toxicity of poisons with parenteral routes of administration]. Toksikologiya novykh promyshlennykh veshchestv, 13, 45–71. [in Russian].

Danilchenko, D. M., & Parchenko, V. V. (2016) Acute toxicity of 5-(furan-2-yl, 2-metylfuran-3-yl)-4-amino-1,2,4-triazole-3-thiol alkyl derivatives. Zaporozhye medical journal, 5(98), 101–104. doi: 10.14739/2310-1210.2016.5.82700.

David, M., Giraudon, I., Mounteney, J., & Dargan, P. (2016) Hospital emergency presentations and acute drug toxicity in Europe. European Monitoring Centre for Drugs, 20. doi: 10.2810/894142.

How to Cite

1.
Аksyonova-Seliuk II, Pruglo YS, Panasenko OI, Knysh YG. The research of acute toxicity of 4-amino-5-(4-(tert-butyl)phenyl)-4H-1,2,4-triazoles-3-thiol derivatives. Current issues in pharmacy and medicine: science and practice [Internet]. 2017Jun.21 [cited 2024Mar.28];(2). Available from: http://pharmed.zsmu.edu.ua/article/view/103771

Issue

Section

Experimental and clinical pharmacology