Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (2): 478-485.DOI: 10.6023/cjoc201705042 Previous Articles     Next Articles



高粟繁a, 许勤龙b, 李家明a, 储昭兴b, 何广卫b, 林高峰b, 朱正伟b,c, 崔勇b,c, 莫佳佳b, 郭敬b, 赵炎b   

  1. a 安徽中医药大学药学院 合肥 230001;
    b 合肥医工医药有限公司 合肥 230001;
    c 安徽医科大学第一附属医院 合肥 230001
  • 收稿日期:2017-05-31 修回日期:2017-09-23 发布日期:2017-10-11
  • 通讯作者: 李家明
  • 基金资助:


Design, Synthesis, and Biological Evaluation of Novel PDE-4 Inhibitors

Gao Sufana, Xu Qinlongb, Li Jiaminga, Chu Zhaoxingb, He Guangweib, Lin Gaofengb, Zhu Zhenweib,c, Cui Yongb,c, Mo Jiajiab, Guo Jingb, Zhao Yanb   

  1. a College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230038;
    b Anhui Medical and Pharmaceutical Co., Ltd, Hefei 230001;
    c First Affiliated Hospital of Anhui Medical University, Hefei 230001
  • Received:2017-05-31 Revised:2017-09-23 Published:2017-10-11
  • Contact: 10.6023/cjoc201705042
  • Supported by:

    Project supported by the National Science and Technology Major Project in 12th Five-Year (No. 2012ZX09401-006).

Based on the reported phosphodiesterase-4(PDE-4) inhibitor of crisaborole, seven compounds with structural novelty were designed and synthesized according to the pharmacophore-combination strategy. The structures of them were identified by NMR and HRMS. Their inhibitory activities against phosphodiesterase-4A (PDE-4A) have been investigated. The inhibitory activities of inflammatory factor induced by lipopolysaccharide (LPS) or phorbol ester have been measured by mouse model. The results showed that all compounds exhibited high anti-inflammatory activities. In particular, one compound activity was significantly better than that of positive control drug.

Key words: PDE-4 inhibitor, crisaborole, synthesis, anti-inflammatory