Discovery of triazole derivatives for biofilm disruption, anti-inflammation and metal ion chelation

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, <b>D</b>) was synthesised efficiently using thiourea as starting material. Finally, the end product <b>E</b> was obtained by aldehyde-amine condensation reaction and the structures of all compounds were determined by spectral analysis. <i>In vitro</i> antimicrobial activity showed that <b>E10</b> had a MIC of 32 μg/mL against the tested <i>Escherichia coli</i> and 16 μg/mL against the tested <i>Staphylococcus aureus</i> strain. Meanwhile, <b>E10</b> has a good anti-biofilm effect. Antibacterial mechanism studies have shown that <b>E10</b> 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, <b>E10</b> 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 Pb²⁺, Cd²⁺, Ca²⁺, Mg²⁺, Fe³⁺,Cr³⁺ and Al³⁺ in the range of 42%-60%.