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ORIGINAL RESEARCH article
Front. Chem.
Sec. Medicinal and Pharmaceutical Chemistry
Volume 13 - 2025 |
doi: 10.3389/fchem.2025.1545259
This article is part of the Research Topic Recent Advances in Synthetic Organic Chemistry at the Biomedical Interface: Honoring Professor Iwao Ojima on the Occasion of his 80th Birthday View all 4 articles
Discovery of triazole derivatives for biofilm disruption, anti-inflammation and metal ion chelation
Provisionally accepted- Department of Pediatrics, Maternity and Child Health Hospital of Qinhuangdao, Qinhuangdao, China
In the face of bacterial hazards to human health and resistance to multiple antibiotics, there is an urgent need to develop new antibiotics to meet the challenge. In this paper, the triazolyl heterocyclic (3-amino-1,2,4-triazole, D) was synthesised efficiently using thiourea as starting material. Finally, the end product E was obtained by aldehyde-amine condensation reaction and the structures of all compounds were determined by spectral analysis. In vitro antimicrobial activity showed that E10 had a MIC of 32 μg/mL against the tested E. coli and 16 μg/mL against the tested S. aureus strain. Meanwhile, E10 has a good anti-biofilm effect. Antibacterial mechanism studies have shown that E10 has a good membrane targeting ability, thus disrupting cell membranes, leading to leakage of intracellular proteins and DNA and accelerating bacterial death. In terms of anti-inflammation, E10 dose-dependently inhibits the levels of inflammatory factors NO and IL-6, which deserves further exploration in the treatment of asthma. The study of metal ion removal capacity showed that the synthesised triazole derivatives have high capacity to remove heavy metals Pb 2+ , Cd 2+ , Ca 2+ , Mg 2+ , Fe 3+ ,Cr 3+ and Al 3+ in the range of 42-60%.
Keywords: 1, 2, 4-triazole derivatives, Anti biofilm, Anti inflammatory, Antiasthmatic, Metal ion detection
Received: 14 Dec 2024; Accepted: 05 Feb 2025.
Copyright: © 2025 Hong, Lu, Tian, Chang, Lu and Gao. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
* Correspondence:
Hongzhi Lu, Department of Pediatrics, Maternity and Child Health Hospital of Qinhuangdao, Qinhuangdao, China
Dawei Tian, Department of Pediatrics, Maternity and Child Health Hospital of Qinhuangdao, Qinhuangdao, China
Yue Chang, Department of Pediatrics, Maternity and Child Health Hospital of Qinhuangdao, Qinhuangdao, China
Qi Lu, Department of Pediatrics, Maternity and Child Health Hospital of Qinhuangdao, Qinhuangdao, China
Feng Gao, Department of Pediatrics, Maternity and Child Health Hospital of Qinhuangdao, Qinhuangdao, China
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