title: 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.
authors.affiliation: Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, PR China.
authors.forename: Xianling
authors.initials: X
authors.lastname: Ning
authors.forename: Ying
authors.initials: Y
authors.lastname: Guo
authors.forename: Xiaoyan
authors.initials: X
authors.lastname: Ma
authors.forename: Renzong
authors.initials: R
authors.lastname: Zhu
authors.forename: Chao
authors.initials: C
authors.lastname: Tian
authors.forename: Zhili
authors.initials: Z
authors.lastname: Zhang
authors.forename: Xiaowei
authors.initials: X
authors.lastname: Wang
authors.forename: Zhizhong
authors.initials: Z
authors.lastname: Ma
authors.forename: Junyi
authors.initials: J
authors.lastname: Liu
mesh_terms: D000818:Animals; D001812:Blood-Brain Barrier / Q000187:drug effects / Q000378:metabolism; D002109:Caffeic Acids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D015195:Drug Design; D016166:Free Radical Scavengers / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051379:Mice; D017628:Microglia / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D018696:Neuroprotective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D009569:Nitric Oxide / Q000378:metabolism; D018384:Oxidative Stress / Q000187:drug effects; D010626:Phenylethyl Alcohol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D013237:Stereoisomerism; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D002109:Caffeic Acids; D016166:Free Radical Scavengers; D018696:Neuroprotective Agents; D013449:Sulfonamides; D009569:Nitric Oxide; C055494:caffeic acid phenethyl ester; D010626:Phenylethyl Alcohol
keywords: (E)-3,4-Dihydroxy styryl sulfonamides; Antioxidants; Blood–brain barrier permeability; Caffeic acid phenethyl ester; Neuroprotective agents