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Synthesis of (1E)-phenyl-2-(3',4'-dihydroxyphenyl)ethenesulfonates as potent neuroprotective agents and evaluation of their activities

Zhutuo Chen, Xianling Ning, Junyi Liu*   

  1. Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
  • Received:2012-12-11 Revised:2013-02-10 Online:2013-03-18 Published:2013-03-18
  • Contact: Junyi Liu*

Abstract:

A series of (1E)-phenyl-2-(3',4'-dihydroxyphenyl)ethenesulfonate derivatives were designed and synthesized as anti-amyotrophic lateral sclerosis (ALS) agents, based on the lead compound caffeic acid phenethyl ester (CAPE). And their neuroprotective activities were evaluated. The results indicated that replacement of the carboxylic ester by sulfonic ester did not produce better neuroprotective activity in the model of LPS induced inflammation in BV2 cells. However, the results in the model of H2O2 induced damage in PC12 cells showed that the neuroprotective activities of all the target compounds and CAPE were about the same.

Key words: Caffeic acid phenethyl ester, Phenylethene sulfonate, Neuroprotection

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