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Published on:June 2018
Indian Journal of Pharmaceutical Education and Research, 2018; 52(3):505-513
Original Article | doi:10.5530/ijper.52.3.58

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


Authors and affiliation (s):

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. Conclusions: 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.

Key words: Synthesize, Anti-inflammatory, RAW 264.7 cell, IL-6.

 

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The Official Journal of Association of Pharmaceutical Teachers of India (APTI)
(Registered under Registration of Societies Act XXI of 1860 No. 122 of 1966-1967, Lucknow)

Indian Journal of Pharmaceutical Education and Research (IJPER) [ISSN-0019-5464] is the official journal of Association of Pharmaceutical Teachers of India (APTI) and is being published since 1967.

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IJPER uses reference linking service using Digital Object Identifiers (DOI) by Crossref. Articles from the year 2013 are being assigned DOIs for its permanent URLs