Synthesis and anti-inflammatory activity evaluation of 5-(1-benzyl-1H-[1,2,3]triazol-4-yl)-4-phenyl-4H-[1,2,4]triazole-3-thiol derivatives

Abstract

Context: Aims: In order to search new compounds with higher anti-inflammatory activities and lower toxicity. 1,2,3-triazole and 1,2,4-triazole derivatives were designed and synthesized, and then the anti-inflammatory activities (in vitro) were evaluated. Settings and Design: The triazole derivatives were designed on the basis of association principle. Methods and Material: 19 benzo[d]-5-(1-Benzyl-1H-[1,2,3]triazol-4-yl)-4-phenyl-4H-[1,2,4]triazole-3-thiol derivatives were synthesized and evaluated for their bioactivities in vitro as anti-inflammatory agents. Statistical analysis used: Statistical analysis was performed by one-way analysis of variance (ANOVA) followed by a least signifcant difference (LSD) test for multiple comparisons, using SPSS version 17.0 statistical software. Results: The results of this study indicated that compound 17(1-Benzyl-4-[5-(4-chloro-phenylsulfanyl)-4-phenyl-4H-[1,2,4]triazol-3-yl]-1H-[1,2,3] triazole) showed excellent inhibition on the expression of IL-6 among these compounds in LPS-induced RAW 264.7 macrophage cell. Conclusion: The findings of this study showed that compound 17 showed excellent inhibition on the expression of IL-6 in LPS-induced macrophage cells. Further studies are warranted to investigate the mechanism of anti-inflammation, in order to represent a novel strategy for the modulation of inflammatory responses.