2. Academic Validation
  3. Design, synthesis and pharmacological evaluation of (E)-3,4-dihydroxy styryl sulfonamides derivatives as multifunctional neuroprotective agents against oxidative and inflammatory injury

Design, synthesis and pharmacological evaluation of (E)-3,4-dihydroxy styryl sulfonamides derivatives as multifunctional neuroprotective agents against oxidative and inflammatory injury

  • Bioorg Med Chem. 2013 Sep 1;21(17):5589-97. doi: 10.1016/j.bmc.2013.05.043.
Xianling Ning 1,  Ying Guo,  Xiaoyan Ma,  Renzong Zhu,  Chao Tian,  Zhili Zhang,  Xiaowei Wang,  Zhizhong Ma,  Junyi Liu
Affiliations

Affiliation

  • 1 Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, PR China.
PMID: 23870700 DOI: 10.1016/j.bmc.2013.05.043
Abstract

A novel class of (E)-3,4-dihydroxy styryl sulfonamides and their 3,4-diacetylated derivatives as caffeic acid phenethyl ester (CAPE) analogs was designed and prepared for improving stability and solubility of the lead compound. Their neuroprotective properties were assessed by several models. The results showed that target compounds displayed positive free radical quenching abilities, superior to that of CAPE. Compounds 6j-k and 7j-k demonstrated remarkable protection effects against damage induced by hydrogen peroxide which were apparently stronger than that of CAPE. Most of target compounds could inhibit nitric oxide production. Additionally, target compounds showed high blood-brain barrier permeability.

Keywords

(E)-3,4-Dihydroxy styryl sulfonamides; Antioxidants; Blood–brain barrier permeability; Caffeic acid phenethyl ester; Neuroprotective agents.

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