Article · Volume 52, Issue 3 · pp. 505–513
Synthesis and Anti-Inflammatory Activity Evaluation of 5-(1-Benzyl-1H-[1,2,3]Triazol-4-yl)-4-Phenyl4H-[1,2,4]Triazole-3-Thiol Derivatives
Chunyan Liu1, Min Bian1,2, Lijun Yu1,2, Chengxi Wei1,2
- 1Medicinal Chemistry and Pharmacology Institute, Inner Mongolia University for the Nationalities, Tongliao, Inner Mongolia, P.R. CHINA.
- 2Inner Mongolia Key Laboratory of Mongolian Medicine Pharmacology for Cardio-Cerebral Vascular System, Tongliao, Inner Mongolia, P.R. CHINA.
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 LPSinduced 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.
Keywords: Synthesize; Anti-inflammatory; RAW 264.7 cell; IL-6
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