Citation: Zhang Qing-Wei, Jiang Ling, Wang Guan, Li Jian-Qi. Design, synthesis and neuroprotective effects of Fenazinel derivatives[J]. Chinese Chemical Letters, ;2017, 28(7): 1505-1508. doi: 10.116/j.cclet.2017.02.003 shu

Design, synthesis and neuroprotective effects of Fenazinel derivatives

Zhang Qing-Wei ^a,b,*,, ,
Jiang Ling ^a,b,c ,
Wang Guan ^a,b ,
Li Jian-Qi ^a,b,*,,

a.
Novel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry, Shanghai 201203, China
b.
Shanghai Engineering Research Center of Pharmaceutical Process, Shanghai 201203, China
c.
School of Engineering, China Pharmaceutical University, Nanjing 211198, China

Corresponding author: Zhang Qing-Wei, sipiqingwei@163.com Li Jian-Qi, lijianqb@126.com

Received Date: 24 November 2016
Revised Date: 23 December 2016
Accepted Date: 16 January 2017
Available Online: 4 July 2017

Figures(3)

In search of novel neuroprotective agents with higher potency and lower hERG liability, a series of novel Fenazinel derivatives were designed and synthesized, among which compounds 8m-o containing amide moiety exhibited good neuroprotective effects in vitro and in vivo. Especially, the representative compound 8o showed lower activity in a patch clamp hERG K⁺ ion channel screen and could be considered as a lead compound for further development. These findings provided an alternative approach to the development of drugs more potent than Fenazinel for the intervention of ischemic stroke.
- Fenazinel,
- Synthesis,
- hERG,
- Neuroprotective,
- Ischemic stroke
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