Abstract
The aim of this research was to investigate the antimicrobial activity of some new 5-(furan-2-yl)-4-amino-1,2,4-triazole-3-thiol substituents and in some cases to trace the relationship between activity of compounds and their structure. Research materials and methods. Antimicrobial activity of new 5-(furan-2-yl)-4-amino-1,2,4-triazole-3-thiol derivatives was studied by the method of serial dilutions. The primary antimicrobial activity screening tests of some 5-(furan-2-yl)-4-amino-1,2,4-triazole-3-thiol derivatives have been conducted on standard test cultures of both gram-positive and gram-negative bacteria that belong to clinically significant group of infectious agents with different morphological properties. Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853 were taken as the set of standard test strains. Results and their discussion. The most sensitive strain was a strain of S. aureus ATCC 25923. Extension of alkyl substituents by the Sulfur atom does not lead to gradual changes in activity but the introduction of pentyl radical increases the activity of a molecule in two times. The transition from the S-alkyl derivatives of 5-(furan-2-yl)-4-amino-1,2,4-triazole-3-thiol to 2-((5-(furan-2-yl)-4-amino-1,2,4-triazole-3-yl)-thio)acetic acid esters doesn’t lead to radical changes of antimicrobial activity and is not drawn. But the introduction of isopropyl and isobutyl radicals in the ester structure of these molecules leads to a sharp increase in activity towards S. aureus ATCC 25923. Conclusions. We have explored antimicrobial activity of new 5-(furan-2-yl)-4-amino-1,2,4-triazole-3-thiol alkyl derivatives and 2-((5-(furan-2-yl)-4-amino-1,2,4-triazole-3-yl)thio)acetic acid esters. It was found that all ten compounds exhibit moderate activity. Some influence of studied substituents on the antimicrobial activity results was also found.
Highlights
Successes of global synthetic organic chemistry which cover study areas of heterocyclic systems properties is the most clearly represented in the modern scientific community
Through a comparative analysis of the availability of the new antimicrobial 5-(furan-2-yl)-4-amino-1,2,4-triazole3-thiol alkyl derivatives and some esters of 2-((5-(furan-2yl)-4-amino-1,2,4-triazole-3-yl)-thio)acetate acid it should be mentioned that striking manifestations of antimicrobial activity of ten represented compounds were not found in reference to comparison drug
The introduction of isopropyl (9, Table 2) and isobutyl (10, Table 2) radicals in the ester structure of these molecules leads to a sharp increase in activity towards S. aureus ATCC 25923
Summary
Successes of global synthetic organic chemistry which cover study areas of heterocyclic systems properties is the most clearly represented in the modern scientific community. Combining different “heterocycles-pharmacophores” together is the actual trend among scientists today. This combining in its turn can lead to a number of compounds with unique properties. 1,2,4-triazole system deserves special attention, because in combination with various five-membered, six-membered heterocycles, aromatic, aliphatic substituents it forms series of various prospect compounds [1]. There is a whole “galaxy” of drugs the active ingredients of which are 1,2,4-triazole derivatives [2]. These drugs are used in the practice of domestic veterinary and medicine. It is recommended by manufacturer “Brovafarma” to use for broiler chickens in the oral dosage forms
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