Synthesis and Biological Activity of Aldehyde Derivatives of Isopimaric Acid

编号 020037005

推送时间 20221121

研究领域 林产化工 

年份 2022 

类型 期刊 

语种 英语

标题 Synthesis and Biological Activity of Aldehyde Derivatives of Isopimaric Acid

来源期刊 MACROHETEROCYCLES

期 第370期

发表时间 20210901

关键词 Synthesis;  characterizationi;  sopimaric acid;  heterocyclic acylhydrazone;  derivatives;  antibacterial activity;  antitumorial activity; 

摘要 Four series of acylhydrazone derivatives, including halogenated aryl modified acylhydrazone, thiophene, pyrrole and quinoline, were synthesized and characterized. The minimum inhibitory concentrations of the compounds against five bacteria were determined and most of the compounds displayed some degree of antibacterial activity. Isopimaric acid (pyrrole-3-carboxaldehyde) acylhydrazone (3j) exhibited the most potent activity against Streptococcus pneumonia and Klebsiella Pneumonia, with the minimum inhibitory concentration being 3.91 mu g/mL. The antimicrobial activity against S. pneumoniae was improved when the pyrrole structure was introduced into isopimaric acid. All heterocyclic acylhydrazone derivatives of isopimaric acid exhibited a good in vitro antitumorial activity at 100 mu M. It is concluded that the inhibitory effect of isopimaric acid (2-fluoro-6-methoxybenzaldehyde) acylhydrazone (3d) on Hep G2 and isopimaric acid (3-bromothiophene-2-carbaldehyde) acylhydrazone (3g) on Hep G2 and MDAMB 231 is better than that of the positive control 5-fluorouracil (5-FU) (76.51%), which is a widely used clinical anticancer agent, at 100 mu M.

服务人员 尚玮姣

服务院士 宋湛谦

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