广州化学2025，Vol.50Issue(6)：31-36,40,7.DOI:10.16560/j.cnki.gzhx.20250610
带有邻苯二酚醚的苯并咪唑类PDE4抑制剂的合成和活性
Synthesis and Activity of Benzimidazole-based PDE4 Inhibitors with Catechol Ethers
摘要
Abstract
Using 3,4-dihydroxybenzaldehyde as the starting material,3,4-bis(difluoromethoxy)benzaldehyde was first synthesized via a substitution reaction.The key benzimidazole-based intermediates with catechol ethers were then prepared through a ring-forming reaction.Nine target compounds were then prepared from the amidation reaction.1H-NMR,13C-NMR,and HRMS were used to characterize and confirm the structures of the target compounds.Investigation into the bioactivities against the PDE4 enzyme showed that the target compounds had strong inhibitory effects on the PDE4 enzyme.The LPS-induced Raw264.7 cell model was then used to evaluate the anti-inflammatory properties,and as a result compound 4f could considerably suppress the increase of NO.关键词
苯并咪唑/磷酸二酯酶 4/抗炎活性/一氧化氮(NO)/分子对接Key words
benzimidazole/phosphodiesterase 4/anti-inflammatory activity/NO/molecular docking分类
医药卫生引用本文复制引用
钱旭东,李刚,耿妍,周绮,陈文华,姚宏亮..带有邻苯二酚醚的苯并咪唑类PDE4抑制剂的合成和活性[J].广州化学,2025,50(6):31-36,40,7.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）
