Abstract

Derivatives of 1,2,4-triazole is a very perspective class of heterocyclic compounds which have high therapeutic effectiveness. The main direction of research on these derivatives are antifungal, antiviral, antibacterial, soothing, hypnotic, anticonvulsant, anti-inflammatory and other activities.
 The aim was to analyze literature data and generalize recent advances in the study of antimicrobial and antifungal action of 1,2,4-triazole derivatives which can help to create new biologically active substances of this type of activity. Bibliosemantical method, systems thinking and the results of our own research were used in the work.
 The results of the literature review of antimicrobial and antifungal activity among new alkyl, aryl and heteryl derivatives of 1,2,4-triazole and among complex compounds, which contain 1,2,4-triazole are as ligands were analyzed and systematized. Some dependence of this type of activity on specialty of chemical structure of heterocyclic system derivatives was specified.
 Perspective of purposeful synthesis of new derivatives of 1,2,4-triazole and products of their transformation as available object for studying biological activity and expanding knowledge about antimicrobial and antifungal activity of this class of heterocyclic compounds were shown with informational analysis. Topicality and practical importance of finding biologically active compounds and receiving biologically active substance by synthesis of new derivatives of 1,2,4-triazole with high antimicrobial activity in relation to gram-negative and gram-positive bacteria were demonstrated.

Highlights

  • The results of the literature review of antimicrobial and antifungal activity among new alkyl, aryl and het­ eryl derivatives of 1,2,4-triazole and among complex compounds, which contain 1,2,4-triazole are as ligands were analyzed and systematized

  • Дослідження синтезованих сполук виконували відносно грампозитивних (S. aureus, B. subtilis, M. luteus), грамнегативних (B. proteus, E. coli, P. aeruginosa, B. typhi) штамів та відносно грибів (C. albicans, C. mycoderma)

  • Висновки Таким чином, провівши інформаційний аналіз треба зазначити, що низка нових синтезованих похідних 1,2,4-триазолу виявляє широкий спектр протимікробної дії

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Summary

Introduction

The results of the literature review of antimicrobial and antifungal activity among new alkyl, aryl and het­ eryl derivatives of 1,2,4-triazole and among complex compounds, which contain 1,2,4-triazole are as ligands were analyzed and systematized. Основними представниками 1,2,4-триазолу, що мають протигрибкову дію є вориконазол [1], флуконазол [2, 3] та ітраконазол [4]. Шість сполук мали потенційну протимікробну активність проти грампозитивних бактерій (мінімальна концентрація, що припиняла ріст, становила 15,63–500 мкг/мл (MIC)). Деякі сполуки виявили високу активність, особливо проти Bacillus subtilis ATCC 6633 (MIC = 15,63–250 мкг/мл), золотистого стафілокока ATCC 25923 (MIC = 31,25– 250 мкг/мл) та Micrococcus luteus ATCC 10240 (MIC = 125–250 мкг/мл).

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