文献类型：期刊文献

英文题名：Synthesis and Biological Activity of Aldehyde Derivatives of Isopimaric Acid

作者：Lu, Yanju[1,2] Zhao, Zhendong[1,2] Chen, Yuxiang[1,2] Wang, Jing[1,2]

第一作者：卢言菊

通信作者：Lu, YJ[1]

机构：[1]Chinese Acad Forestry, Key Lab Biomass Energy & Mat,Coinnovat Ctr Effici, Inst Chem Ind Forest Prod,Key Lab Chem Engn Fores, Natl Forestry & Grassland Adm,Natl Engn Lab Bioma, Nanjing 210042, Jiangsu, Peoples R China;[2]Chinese Acad Forestry, Res Inst Forestry New Technol, Beijing 100091, Peoples R China

年份：2021

卷号：18

期号：12

起止页码：950-956

外文期刊名：LETTERS IN ORGANIC CHEMISTRY

收录：;Scopus(收录号：2-s2.0-85124477153);WOS:【SCI-EXPANDED(收录号:WOS:000731793300004)】；

基金：This research was supported by the National Natural Sci-ence Foundation of China (grant No. 31700504) and the Fun-damental Research Funds of Jiangsu Province Biomass Energy and Materials Laboratory (grant No. JSBEM-201808) .

语种：英文

外文关键词：Synthesis; characterization; isopimaric 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.