Acute toxicity of 5-(2-, 3-, 4-methoxyphenyl, (3,4,5-trimethoxyphenyl)-)-1,2,4-triazole-3-thiones and its thioderivatives

Authors

  • Yu. G. Samelyuk Zaporizhzhia State Medical University,
  • A. G. Kaplaushenko Zaporizhzhia State Medical University,

DOI:

https://doi.org/10.14739/2409-2932.2015.3.52660

Keywords:

1, 2, 4-triazoles, Acute Toxicity Tests

Abstract

Aim. We have continued the study of 1,2,4-triazole derivatives,  which contain 2-, 3- , 4-methoxyphenyl or 3,4,5- methoxyphenyl substituents in 5th position of the triazole nucleus. An acute toxicity has been investigated for 11 eleven different classes of synthesized compounds based on heterocyclic triazole system.

Methods. Investigations have been carried out using white Wistar rats. Five groups of animals have been used to determine LD50 of 5-R-1,2,4-triazole-3-thiones and its derivatives.  Two observations have been set for each group using a previous dose and the next one. 

Conclusion. The obtained results show that LD50values of new 1,2,4-triazole-3-thiones derivatives which contain methoxyphenyl substituents in 5th position of the triazole nucleus, are in rage 304±65-1245±197 mg/kg. Investigated compounds are low-toxic or non-toxic substances according to Sidorov classification.

The presence and nature of substituents at the 1,2,4-triazole nucleus and nature of substituents connected with Sulfur in third position of 1,2,4-triazole nucleus affect the acute toxicity of 5-R-1,2,4-triazole-3-thiones and its derivatives.

References

Kaplaushenko, A. H. (2007) Budova ta hostra toksychnist amino- i tio- pokhidnykh 1,2,4-triazolu [Acute toxicity of amino- and tio-derivatives of 1,2,4-triazole]. Farmatsevtychnyi zhurnal. – 2007(1/40), 104–107. [in Ukrainian].

Kaplaushenko, A. G. (2010) Vzaiemozviazok mizh hostroiu toksychnistiu i doslidzhenymy vydamy farmakolohichnoi aktyvnosti 4-mono- i 4,5-dyzamishchenykh 1,2,4-triazol-3-tionu ta yikh S-pokhidnykh [Relationships between the acute toxicity and studied types of pharmacological activity parameters of the 4-mono- and 4,5-disubstituted 1,2,4-

triazole-3-thione and their thioderivatives]. Zaporozhskij medicinkij zhurnal, 12(4), 80–82. [in Ukrainian].

Kaplaushenko, A. H. (2006) Syntez, fizyko-khimichni ta biolohichni vlastyvosti S-pokhidnykh 5-(2-, 3-, 4-nitrofenil)-1,2,4-triazol-3-tioniv (Dis… kand. farm. nauk). [Synthesis, physical, chemical and biological properties of S-derivatives of 5-(2-, 3-, 4-nitrophenyl)-1,2,4-triazole-3-thiones. Dr. farm. sci. diss.]. Kyiv. [in Ukrainian].

Prozorovskij, V. B. (1960) O vybore metoda postroeniya krivoj letal′nosti i opredelenie srednej letal′noj dozy [On the choice of the method of constructing mortality curve and determination of the mean lethal dose]. Zhurnal obschej biologii, 21(3), 221–228. [in Russian].

Panasenko, O. I. (2005) Syntez, peretvorennia, fizyko-khimichni ta biolohichni vlastyvosti pokhidnykh 1,2,4-triazolu (Dis… dokt. farm. nauk). [Synthesis, transformation, physico-chemical and biological properties of derivatives of 1,2,4- triazoles. Dr. farm. sci. diss.]. Kyiv. [in Ukrainian].

Parchenko, V. V. (2006) Syntez, fizyko-khimichni ta biolohichni vlastyvosti 1,2,4-triazol-3-tioniv, shcho mistiat yadro furanu (Dis. kand. farm. nauk). [Synthesis, physico-chemical and biological properties of 1,2,4- triazoles -3- thiones containing core furan. Dr. farm. sci. diss.]. Kyiv. [in Ukrainian].

Sidorov, K. K. (1973) O klassifikacii toksichnosti yadov pri parenteral′nykh sposobakh vvedeniya [The classification of toxic poisons in the parenteral route of administration]. Toksikologiya novyh promyshlennykh veschestv, 13, 45–71. [in Russian].

Downloads

How to Cite

1.
Samelyuk YG, Kaplaushenko AG. Acute toxicity of 5-(2-, 3-, 4-methoxyphenyl, (3,4,5-trimethoxyphenyl)-)-1,2,4-triazole-3-thiones and its thioderivatives. Current issues in pharmacy and medicine: science and practice [Internet]. 2015Nov.3 [cited 2024Dec.25];(3). Available from: http://pharmed.zsmu.edu.ua/article/view/52660

Issue

No. 3 (2015)

Section

Experimental and clinical pharmacology

License

Authors who publish with this journal agree to the following terms:

    1. 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.     Лицензия Creative Commons
    2. 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.
    3. 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)