Synthesis and antimicrobial activity of derivatives of 4-amino-5-(4-tertbutylphenyl)-4H-1,2,4-triazole-3-thiol

  • I. Aksenova Zaporizhzhia State Medical University
  • A. Рanasenko Zaporizhzhia State Medical University
  • E. Knysh Zaporizhzhia State Medical University
  • N. Polishchuk Zaporizhzhia State Medical University
Keywords: organic synthesis, triazoles, antimicrobial activity

Abstract

Wide and uncontrolled use of antibiotics and antimicrobial drugs among the population led to increase of resistance of microorganisms. So even slight infections and injuries can lead to serious consequences.

Analysis of the current literature of organic synthesis showed that one of the most promising classes for synthesis of new drugs is the class of 1,2,4-triazole.

This class of chemical compounds is well established in clinical practice owing to wide spectrum of biological activities (antimicrobial, hypotensive, antispasmodic, etc.) and a small amount of side effects.

The aim of the work is the synthesis of new compounds – derivatives of 4-amino-5-(4-tertbutylphenyl)-4H-1,2,4-triazole-3-thiol, investigation of their antimicrobial properties and establishment certain patterns of dependence «structure–action».

Objects of investigations were the salt – the derivatives of 4-amino-5-(4-tertbutylphenyl)-4H-1,2,4-triazole-3-thiol. During the work elemental analysis, chromatography-mass-spectrometric investigation, 1H-NMR spectroscopy, the methods of synthesis and were carried out and was investigated the antimicrobial activity of the test compounds.

Researches have established some dependence «structure–action» and have identified compounds whose antimicrobial activity exceeded the indicators of the reference preparation – chlorhexidine.

In the result of researches original methods of synthesis derivatives of 4-amino-5-(4-tertbutylphenyl)-4H-1,2,4-triazole-3-thiol was suggested, promising compounds which exhibit an antimicrobial action was revealed and some regularity «structure–action» was installered.

References

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Published
2019-02-12
How to Cite
Aksenova, I., РanasenkoA., Knysh, E., & Polishchuk, N. (2019). Synthesis and antimicrobial activity of derivatives of 4-amino-5-(4-tertbutylphenyl)-4H-1,2,4-triazole-3-thiol. Farmatsevtychnyi Zhurnal, (6), 62-68. Retrieved from https://pharmj.org.ua/index.php/journal/article/view/274
Section
Synthesis and analysis of biologically active compounds