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

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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Ning X,Guo Y,Ma X,Zhu R,Tian C,Zhang Z,Wang X,Ma Z,Liu J

doi

10.1016/j.bmc.2013.05.043

subject

Has Abstract

pub_date

2013-09-01 00:00:00

pages

5589-97

issue

17

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(13)00492-6

journal_volume

21

pub_type

杂志文章

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