Current research trends of 1,2,4-triazole derivatives biological activity (literature review)
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| Název: | Current research trends of 1,2,4-triazole derivatives biological activity (literature review) |
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| Autoři: | I. M. Bilai, V. I. Dariy, A. V. Khilkovets, A. I. Bilai |
| Zdroj: | Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki, Vol 18, Iss 2, Pp 197-205 (2025) |
| Informace o vydavateli: | Zaporizhzhia State Medical and Pharmaceutical University, 2025. |
| Rok vydání: | 2025 |
| Témata: | RS1-441, derivatives 1, Pharmacy and materia medica, biological activity, 4-triazole |
| Popis: | The relevance of searching for new active compounds among 1,2,4-triazole derivatives is determined by their potential effectiveness in treating various diseases such as cancer, inflammation, microbial infections, and antioxidant disorders. Studies show that these compounds can inhibit the proliferation of cancer cells, exhibit anti-inflammatory properties, demonstrate activity against pathogenic microorganisms, and neutralize free radicals, which is important for preventing oxidative stress. Therefore, the study of 1,2,4-triazole derivatives may lead to the development of new effective drugs, which is extremely relevant in modern medicine. The aim of the work is to summarize recent scientific advances in the study of 1,2,4-triazole derivatives, particularly their antitumor, antimicrobial, anti-inflammatory, anticonvulsant, and antioxidant activity, to substantiate their potential as multifunctional therapeutic agents in modern medicine. Results. The literature review confirmed that 1,2,4-triazole derivatives exhibit significant biological activity across various therapeutic areas. Studies revealed high antitumor efficacy of hybrid compounds, particularly the derivative 5-((4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)methyl)-4-(4-nitrophenyl)-4H-1,2,4-triazole-3-thiol, which demonstrated notable activity against breast cancer cells (MCF-7), as confirmed by DFT and molecular docking methods. In antimicrobial therapy, derivatives combined with norfloxacin showed higher efficacy compared to standard antibiotics against both Gram-positive and Gram-negative bacteria while maintaining good biocompatibility. Research on anticonvulsant properties found that 4-amino-4H-1,2,4-triazole derivatives effectively interact with the GABA-A receptor, outperforming the standard drug phenytoin in in vivo models. In anti-inflammatory studies, compounds containing a 1,3,4-thiadiazine fragment achieved 91 % inhibition of edema, surpassing ibuprofen (82 %), and reduced key inflammatory biomarkers. The antioxidant properties of brominated [1,2,4]triazolo[1,5-a]pyridine derivatives were particularly pronounced, with maximum activity observed at a concentration of 150 μg/mL. These results highlight the broad therapeutic potential of 1,2,4-triazole derivatives, making them promising candidates for the development of novel drugs to combat oncological, infectious, inflammatory, and neurodegenerative diseases, as well as for oxidative stress prevention. Conclusions. 1,2,4-Triazole derivatives exhibit a wide range of biological activity, including antifungal, antimicrobial, anticancer, antibacterial, anticonvulsant, anti-inflammatory, and antioxidant properties. This indicates their potential as versatile agents for the treatment of various diseases. |
| Druh dokumentu: | Article |
| ISSN: | 2409-2932 2306-8094 |
| DOI: | 10.14739/2409-2932.2025.2.322344 |
| Přístupová URL adresa: | https://doaj.org/article/800b2ec27329456bac5b1f732ec7a91c https://doi.org/10.14739/2409-2932.2025.2.322344 |
| Rights: | CC BY |
| Přístupové číslo: | edsair.doi.dedup.....51dcabaa1ba700ba36ed8b101d9ca4fe |
| Databáze: | OpenAIRE |
Nájsť tento článok vo Web of Science | Abstrakt: | The relevance of searching for new active compounds among 1,2,4-triazole derivatives is determined by their potential effectiveness in treating various diseases such as cancer, inflammation, microbial infections, and antioxidant disorders. Studies show that these compounds can inhibit the proliferation of cancer cells, exhibit anti-inflammatory properties, demonstrate activity against pathogenic microorganisms, and neutralize free radicals, which is important for preventing oxidative stress. Therefore, the study of 1,2,4-triazole derivatives may lead to the development of new effective drugs, which is extremely relevant in modern medicine. The aim of the work is to summarize recent scientific advances in the study of 1,2,4-triazole derivatives, particularly their antitumor, antimicrobial, anti-inflammatory, anticonvulsant, and antioxidant activity, to substantiate their potential as multifunctional therapeutic agents in modern medicine. Results. The literature review confirmed that 1,2,4-triazole derivatives exhibit significant biological activity across various therapeutic areas. Studies revealed high antitumor efficacy of hybrid compounds, particularly the derivative 5-((4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)methyl)-4-(4-nitrophenyl)-4H-1,2,4-triazole-3-thiol, which demonstrated notable activity against breast cancer cells (MCF-7), as confirmed by DFT and molecular docking methods. In antimicrobial therapy, derivatives combined with norfloxacin showed higher efficacy compared to standard antibiotics against both Gram-positive and Gram-negative bacteria while maintaining good biocompatibility. Research on anticonvulsant properties found that 4-amino-4H-1,2,4-triazole derivatives effectively interact with the GABA-A receptor, outperforming the standard drug phenytoin in in vivo models. In anti-inflammatory studies, compounds containing a 1,3,4-thiadiazine fragment achieved 91 % inhibition of edema, surpassing ibuprofen (82 %), and reduced key inflammatory biomarkers. The antioxidant properties of brominated [1,2,4]triazolo[1,5-a]pyridine derivatives were particularly pronounced, with maximum activity observed at a concentration of 150 μg/mL. These results highlight the broad therapeutic potential of 1,2,4-triazole derivatives, making them promising candidates for the development of novel drugs to combat oncological, infectious, inflammatory, and neurodegenerative diseases, as well as for oxidative stress prevention. Conclusions. 1,2,4-Triazole derivatives exhibit a wide range of biological activity, including antifungal, antimicrobial, anticancer, antibacterial, anticonvulsant, anti-inflammatory, and antioxidant properties. This indicates their potential as versatile agents for the treatment of various diseases. |
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| ISSN: | 24092932 23068094 |
| DOI: | 10.14739/2409-2932.2025.2.322344 |