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.
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DOI：
10.1016/j.bmc.2013.05.043
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发表时间：
2013-09
影响因子：
3.5
通讯作者：
Xianling Ning;Ying Guo;Xiaoyan Ma;Renzong Zhu;Chao Tian;Zhili Zhang;Xiaowei Wang;Zhizhong Ma;
中科院分区：
文献类型：
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作者：
Xianling Ning;Ying Guo;Xiaoyan Ma;Renzong Zhu;Chao Tian;Zhili Zhang;Xiaowei Wang;Zhizhong Ma;
设计并合成了一类新型的（E）-3，4-二羟基苯乙烯基磺酰胺及其3，4-二乙酰化衍生物咖啡酸苯乙酯（CAPE）类似物，以改善先导化合物的稳定性和溶解性。通过几种模型评估其神经保护特性。结果表明，目标化合物对自由基具有良好的猝灭作用，其猝灭效果上级于CAPE。化合物6 j-k和7 j-k对过氧化氢诱导的细胞损伤有明显的保护作用，其保护作用明显强于CAPE。大多数目标化合物对一氧化氮的产生有抑制作用。此外，目标化合物显示出高的血脑屏障通透性。
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. Compounds6j–kand7j–kdemonstrated 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.