Antimicrobial and antifungal activity of new 4-(5-((5-(alkylthio)-4-R-4H-1,2,4-triazole-3-yl)thio)-1H-1,2,4-triazole-3-yl)pyridines
The resistance of such strains as Staphylococcus aureus, Escherichia coli extends to many antimicrobial drugs. This problem can be solved by searching for new drugs with high bactericidal and antifungal action. Recent studies have shown the promise of searching for biologically active substances of...
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Zaporizhzhia State Medical and Pharmaceutical University
2020-11-01
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| Series: | Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki |
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| Online Access: | http://pharmed.zsmu.edu.ua/article/view/216204/216801 |
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| author | Ye. O. Karpun N. M. Polishchuk |
| author_facet | Ye. O. Karpun N. M. Polishchuk |
| author_sort | Ye. O. Karpun |
| collection | DOAJ |
| description | The resistance of such strains as Staphylococcus aureus, Escherichia coli extends to many antimicrobial drugs. This problem can be solved by searching for new drugs with high bactericidal and antifungal action. Recent studies have shown the promise of searching for biologically active substances of antimicrobial and antifungal action among 1,2,4-triazole derivatives.
The aim of this work was to develop the antimicrobial and antifungal effects of the homologous series of S-alkyl-substituted 4-R-5-(((3-(pyridin-4-yl)-1H-1,2,4-triazole-5-yl)thio)methyl)-4Н-1,2,4-triazole-3-thiols and draw conclusions regarding the structural and functional relationship of the synthesized compounds.
Materials and methods. The subject of research was 4-(5-(((5-(alkylthio)-4-methyl-4H-1,2,4-triazole-3-yl)thio)-1H-1,2,4-triazole-3-yl)pyridines and 4-(5-(((5-(alkylthio)-4-ethyl-4H-1,2,4-triazole-3-yl)thio)-1H-1,2,4-triazole-3-yl)pyridines. The activity was analyzed by the method of two-fold serial dilutions on test cultures of Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Candida albicans.
The results of the biological screening showed that all tested compounds exhibited antibacterial action (MIC – in the range of 31.25–62.50 μg/ml, MBС – in the range of 62.5–125.0 μg/ml) and antifungal effect (MIC – in within 31.25–62.50 μg/ml, MFС – within 62.5–125.0 μg/ml) relative to the control. The obtained compounds exhibit more pronounced activity against the Pseudomonas aeruginosa strain (MIC – in the range of 31.25–62.50 μg/ml, MBcС – in the range of 62.5–125.0 μg/ml) and antifungal activity against the Candida albicans strain (MIC – within 31.25–62.50 μg/ml, MFС – within 62.5–125.0 μg/ml) relative to the control.
Conclusions. The biological screening data indicate that the search among the given bis-1,2,4-triazole derivatives is promising. The most active among the series of S-alkyl-substituted 4-R-5-(((3-(pyridin-4-yl)-1Н-1,2,4-triazole-5-yl)thio)methyl)-4Н-1,2,4-triazole-3-thiols was compound 4-(5-(((4-methyl-5-(pentylthio)-4H-1,2,4-triazole-3-yl)thio)-1H-1,2,4-triazole-3-yl)pyridine, which exhibited the most pronounced antimicrobial effect against the Staphylococcus aureus strain (MIC – 15.6 μg/ml, MBС – 31.25 μg/ml) indicate the prospects of searching in the specified number of substituted. |
| format | Article |
| id | doaj-art-12a4f4c629cc4848ade764bd8494af2f |
| institution | DOAJ |
| issn | 2306-8094 2409-2932 |
| language | English |
| publishDate | 2020-11-01 |
| publisher | Zaporizhzhia State Medical and Pharmaceutical University |
| record_format | Article |
| series | Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki |
| spelling | doaj-art-12a4f4c629cc4848ade764bd8494af2f2025-08-20T02:42:01ZengZaporizhzhia State Medical and Pharmaceutical UniversityAktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki2306-80942409-29322020-11-0113335435810.14739/2409-2932.2020.3.216204Antimicrobial and antifungal activity of new 4-(5-((5-(alkylthio)-4-R-4H-1,2,4-triazole-3-yl)thio)-1H-1,2,4-triazole-3-yl)pyridinesYe. O. Karpun0https://orcid.org/0000-0003-1816-812X N. M. Polishchuk1https://orcid.org/0000-0002-9791-5818 Zaporizhzhia State Medical University, UkraineZaporizhzhia State Medical University, UkraineThe resistance of such strains as Staphylococcus aureus, Escherichia coli extends to many antimicrobial drugs. This problem can be solved by searching for new drugs with high bactericidal and antifungal action. Recent studies have shown the promise of searching for biologically active substances of antimicrobial and antifungal action among 1,2,4-triazole derivatives. The aim of this work was to develop the antimicrobial and antifungal effects of the homologous series of S-alkyl-substituted 4-R-5-(((3-(pyridin-4-yl)-1H-1,2,4-triazole-5-yl)thio)methyl)-4Н-1,2,4-triazole-3-thiols and draw conclusions regarding the structural and functional relationship of the synthesized compounds. Materials and methods. The subject of research was 4-(5-(((5-(alkylthio)-4-methyl-4H-1,2,4-triazole-3-yl)thio)-1H-1,2,4-triazole-3-yl)pyridines and 4-(5-(((5-(alkylthio)-4-ethyl-4H-1,2,4-triazole-3-yl)thio)-1H-1,2,4-triazole-3-yl)pyridines. The activity was analyzed by the method of two-fold serial dilutions on test cultures of Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Candida albicans. The results of the biological screening showed that all tested compounds exhibited antibacterial action (MIC – in the range of 31.25–62.50 μg/ml, MBС – in the range of 62.5–125.0 μg/ml) and antifungal effect (MIC – in within 31.25–62.50 μg/ml, MFС – within 62.5–125.0 μg/ml) relative to the control. The obtained compounds exhibit more pronounced activity against the Pseudomonas aeruginosa strain (MIC – in the range of 31.25–62.50 μg/ml, MBcС – in the range of 62.5–125.0 μg/ml) and antifungal activity against the Candida albicans strain (MIC – within 31.25–62.50 μg/ml, MFС – within 62.5–125.0 μg/ml) relative to the control. Conclusions. The biological screening data indicate that the search among the given bis-1,2,4-triazole derivatives is promising. The most active among the series of S-alkyl-substituted 4-R-5-(((3-(pyridin-4-yl)-1Н-1,2,4-triazole-5-yl)thio)methyl)-4Н-1,2,4-triazole-3-thiols was compound 4-(5-(((4-methyl-5-(pentylthio)-4H-1,2,4-triazole-3-yl)thio)-1H-1,2,4-triazole-3-yl)pyridine, which exhibited the most pronounced antimicrobial effect against the Staphylococcus aureus strain (MIC – 15.6 μg/ml, MBС – 31.25 μg/ml) indicate the prospects of searching in the specified number of substituted.http://pharmed.zsmu.edu.ua/article/view/216204/2168011 2 4-triazoleantimicrobial activityantifungal activity |
| spellingShingle | Ye. O. Karpun N. M. Polishchuk Antimicrobial and antifungal activity of new 4-(5-((5-(alkylthio)-4-R-4H-1,2,4-triazole-3-yl)thio)-1H-1,2,4-triazole-3-yl)pyridines Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki 1 2 4-triazole antimicrobial activity antifungal activity |
| title | Antimicrobial and antifungal activity of new 4-(5-((5-(alkylthio)-4-R-4H-1,2,4-triazole-3-yl)thio)-1H-1,2,4-triazole-3-yl)pyridines |
| title_full | Antimicrobial and antifungal activity of new 4-(5-((5-(alkylthio)-4-R-4H-1,2,4-triazole-3-yl)thio)-1H-1,2,4-triazole-3-yl)pyridines |
| title_fullStr | Antimicrobial and antifungal activity of new 4-(5-((5-(alkylthio)-4-R-4H-1,2,4-triazole-3-yl)thio)-1H-1,2,4-triazole-3-yl)pyridines |
| title_full_unstemmed | Antimicrobial and antifungal activity of new 4-(5-((5-(alkylthio)-4-R-4H-1,2,4-triazole-3-yl)thio)-1H-1,2,4-triazole-3-yl)pyridines |
| title_short | Antimicrobial and antifungal activity of new 4-(5-((5-(alkylthio)-4-R-4H-1,2,4-triazole-3-yl)thio)-1H-1,2,4-triazole-3-yl)pyridines |
| title_sort | antimicrobial and antifungal activity of new 4 5 5 alkylthio 4 r 4h 1 2 4 triazole 3 yl thio 1h 1 2 4 triazole 3 yl pyridines |
| topic | 1 2 4-triazole antimicrobial activity antifungal activity |
| url | http://pharmed.zsmu.edu.ua/article/view/216204/216801 |
| work_keys_str_mv | AT yeokarpun antimicrobialandantifungalactivityofnew455alkylthio4r4h124triazole3ylthio1h124triazole3ylpyridines AT nmpolishchuk antimicrobialandantifungalactivityofnew455alkylthio4r4h124triazole3ylthio1h124triazole3ylpyridines |