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Chinese Journal of Organic Chemistry >

2018 , Vol. 38 >Issue 2: 478 - 485

DOI: https://doi.org/10.6023/cjoc201705042

Articles

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

  • Gao Sufan ,
  • Xu Qinlong ,
  • Li Jiaming ,
  • Chu Zhaoxing ,
  • He Guangwei ,
  • Lin Gaofeng ,
  • Zhu Zhenwei ,
  • Cui Yong ,
  • Mo Jiajia ,
  • Guo Jing ,
  • Zhao Yan
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  • 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 date: 2017-05-31

  Revised date: 2017-09-23

  Online published: 2017-10-11

Supported by

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

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Abstract

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

Cite this article

Gao Sufan , Xu Qinlong , Li Jiaming , Chu Zhaoxing , He Guangwei , Lin Gaofeng , Zhu Zhenwei , Cui Yong , Mo Jiajia , Guo Jing , Zhao Yan . Design, Synthesis, and Biological Evaluation of Novel PDE-4 Inhibitors[J]. Chinese Journal of Organic Chemistry, 2018 , 38(2) : 478 -485 . DOI: 10.6023/cjoc201705042

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