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Synthesis of bioactive 1,4-disubstituted 1,2,3-triazole-linked Thiosemicarbazone derivatives using Cu2O microbeads catalysis for enhanced antibacterial and antioxidant activities
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Synthesis of bioactive 1,4-disubstituted 1,2,3-triazole-linked Thiosemicarbazone derivatives using Cu2O microbeads catalysis for enhanced antibacterial and antioxidant activities

Halla Abdelbaki, Amar Djemoui, Mohammed Ridha Ouahrani, Mohammed Messaoudi, Ilham Ben Amor, Huda Alsaeedi, David Cornu, Mikhael Bechelany et Ahmed Barhoum
Journal of Molecular Structure, Vol.1324
03/2025

Résumé

1 2 3-triazole Thiosemicarbazone DPPH Antibacterial activity Antioxidant activity ABTS Structure-activity relationship
This study focuses on the design, synthesis and evaluation of antibacterial and antioxidant properties of 1,4-disubstituted 1,2,3-triazole-linked thiosemicarbazone derivatives.The synthesis involved a multistep process, beginning with the preparation of alkyne derivatives from three benzaldehyde derivatives (4-hydroxybenzaldehyde, vanillin, and salicylaldehyde) and using flower-like Cu2O microbeads as a catalyst. The synthesized compounds were evaluated for antibacterial activity against four bacterial strains: Escherichia coli (E. coli), Pseudomonas aeruginosa (P. aeruginosa), Bacillus subtilis (B. subtilis), and Staphylococcus aureus (S. aureus), at concentrations ranging from 10 to 80 mg/mL, using ciprofloxacin (CIP) as a reference. Among the derivatives, Compound 3c, (Z)-2-(4-((1-benzyl-1H-1,2,3-triazol-4-yl)methoxy)-3-methoxybenzylidene)hydrazine-1-carbothioamide,exhibited the most potent antibacterial activity against E. coli, with a zone of inhibition of 22±0.1 mm at 80 mg/mL. Compound 3a, (Z)-2-(4-((1-benzyl-1H-1,2,3-triazol-4-yl)methoxy)benzylidene)hydrazine-1-carbothioamide, showed the highest efficacy against B. subtilis, with an inhibition zone of 21±0.4 mm. Antioxidant assays, including DPPH and ABTS, revealed Compound 3c to have the lowest IC50 values (2 ± 0.4 μg/mL and 160±0.1 μg/mL, respectively), indicating strong antioxidant activity. These results demonstrate that Cu2Ocatalyzed synthesis and chemical substitution in 1,4-disubstituted 1,2,3-triazole-linked thiosemicarbazone derivatives significantly enhance their antibacterial and antioxidant activities, making them promising candidates for therapeutic development.

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