Citation: 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 shu

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

Gao Sufan ^a ,
Xu Qinlong ^b ,
Li Jiaming ^a,, ,
Chu Zhaoxing ^b ,
He Guangwei ^b ,
Lin Gaofeng ^b ,
Zhu Zhenwei ^b,c ,
Cui Yong ^b,c ,
Mo Jiajia ^b ,
Guo Jing ^b ,
Zhao Yan ^b

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

Corresponding author: Li Jiaming, lijiaming2004@sina.com
Received Date: 31 May 2017
Revised Date: 23 September 2017
Available Online: 11 February 2018
Fund Project: the National Science and Technology Major Project in 12th Five-Year 2012ZX09401-006Project supported by the National Science and Technology Major Project in 12th Five-Year (No. 2012ZX09401-006)

Figures(8)

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.
- PDE-4 inhibitor,
- crisaborole,
- synthesis,
- anti-inflammatory
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