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- MakaleYalnız künye2026Synthesis, antioxidant, and antiurease activities of novel benzimidazole-based 1,3,4-thiadiazole derivatives
Gümrükçüoğlu, Taner İlker; Akgün, Hakan; Bektaş, Hakan; Sökmen, Bahar Bilgin; Menteşe, Emre
In this study, we report the synthesis and characterisation of five new benzimidazole-based 1, 3, 4-thiadiazole derivatives (5a–e) and the evaluation of their antioxidant and antiurease activities. The structures were confirmed by NMR (1H, 13C) and LC/TOF–MS analyses (spectra are given in the supplementary information). Biological assays (DPPH, ABTS, iron-reducing power, urease inhibition) revealed that compound 5e (bearing a 4-nitrophenyl substituent) exhibited the strongest urease inhibition (EC50 = 0.1296 ± 0.0260 µM), surpassing thiourea. One-way ANOVA revealed significant differences in urease inhibition between the compounds (p<0.001). Post-hoc Tukey tests confirmed that compound 5e was more effective than several other compounds. The compounds exhibited moderate and comparable antioxidant activities. The first SAR study shows that electron-withdrawing substituents increase urease inhibition, whereas electron-donating groups increase the reducing power. Comparison with earlier reported triazole analogues shows scaffold-dependent changes in bioactivity. These findings support thiadiazoles as promising dual-function agents for oxidative stress and urease-associated pathologies.
- MakaleYalnız künye2025Synthesis of New Triazole Compounds: Determination of Antiurease and Antioxidant Activities
Gümrükçüoğlu, T.İ.; Akgün, H.; Sökmen, B. Bilgin; Bektaş, H.
Abstract: Objective: In this study, we synthesized five novel triazole derivatives and biologically evaluated their antiurease and antioxidant properties. Methods: Five novel 1,2,4-triazole derivatives (5a–5e) were synthesized and tested for their urease inhibition and antioxidant activities using spectrophotometric methods. Results and Discussion: All compounds exhibited varying degrees of biological activity, with compound 5c demonstrating the most potent urease inhibition and radical scavenging capacity. Statistical analysis confirmed significant differences among the compounds, particularly highlighting the superior performance of 5c. Conclusions: These results suggest that halogen-substituted triazoles are promising candidates for further pharmacological development aimed at oxidative stress-related conditions and urease-associated pathologies.