广州化学2025，Vol.50Issue(4)：7-14,8.DOI:10.16560/j.cnki.gzhx.20250411
含氮杂环衍生物的设计、合成及抗炎活性研究
Design,Synthesis and Anti-inflammatory Activity of Nitrogen-containing Heterocyclic Derivatives
摘要
Abstract
Starting with 3,4-dihydroxybenzaldehyde,two substitution reactions were carried out to obtain 3-(cyclopropylmethoxy)-4-(difluoromethoxy)benzaldehyde.Then,oxidation and ring-closing reactions were performed to obtain the important intermediate triazole derivative.Finally,amidation reactions were carried out to obtain six target compounds.Additionally,a ring-closing reaction was performed on the triazole derivative to obtain an important intermediate of triazolepyrimidine ring,and then Suzuki coupling reactions were performed to obtain another six target compounds.The structures of the 12 target compounds were confirmed by MS,1H-NMR,and 13C-NMR.The anti-inflammatory effects of the target compounds were tested using LPS-induced Raw264.7 cell inflammation assays,among which 8c exihibited good effect,with IC50 against IL-6 and TNF-α of 39.65 μmol/L and 55.62 μmol/L,respectively.关键词
合成/抗炎/铃木偶联/三氮唑/三氮唑并嘧啶Key words
synthesis/anti-inflammatory/Suzuki coupling/triazole/triazolopyrimidine分类
医药卫生引用本文复制引用
何登芹,欧扬慧,李刚,吴家强,姚宏亮..含氮杂环衍生物的设计、合成及抗炎活性研究[J].广州化学,2025,50(4):7-14,8.基金项目
广东省重点领域研发计划项目(2020B1111580001) （2020B1111580001）
广东省科学院科技发展专项(2022GDASZH-2022010110) （2022GDASZH-2022010110）
