300700-01-0Relevant academic research and scientific papers
Sulfones nitroxyl radical as a radioprotective agent application
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Paragraph 0021; 0023, (2018/05/16)
The invention discloses a sulfone-type nitroxide free radical represented by a structural general formula (I) and an application thereof as a radiation protectant. In the formula, R1 is absent or is halogen, C1-C3 alkyl, C1-C3 alkoxy or -CF3; and R2 is hy
Styryl sulfones compound, its preparation method and its use as neuroprotective agents
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Paragraph 0063-0065; 0122-0124, (2018/02/04)
The application relates to design of a novel molecule with ester group substituted by sulfone group by using a caffeic acid phenethyl ester (CAPE) with neuroprotective activity extracted from natural propolis as a primer according to bioisosterism principle and hydrogen-bond interaction theory; and the molecule has a structural general formula I, and the definition of each group is shown in the claims. The invention also relates to compound in vitroantioxidation capability evaluation, neuroprotective activity evaluation on cell level and traverse blood brain barrier ability evaluation. Activity evaluation results show that the synthesized novel compound has enhanced neuroprotective activity and can easily traverse the blood brain barrier, thus becoming a novel neuroprotective agent for treating neurodegenerative diseases.
Synthesis, characterization, and radioprotective activity of α,β-unsaturated aryl sulfone analogs and their Tempol conjugates
Zhou, Nan,Feng, Tian,Shen, Xin,Cui, Jiahui,Wu, Rangxin,Wang, Libin,Wang, Siwang,Zhang, Shengyong,Chen, Hui
supporting information, p. 1063 - 1068 (2017/07/12)
Some novel α,β-unsaturated aromatic sulfone analogs (5a-5m) and their Tempol conjugates (6a-6e) have been synthetically prepared, characterized and evaluated for their radioprotective activity under γ-ray radiation. The Tempol conjugates were characterize
Design, synthesis, and biological evaluation of (E)-3,4-dihydroxystyryl aralkyl sulfones and sulfoxides as novel multifunctional neuroprotective agents
Ning, Xianling,Guo, Ying,Wang, Xiaowei,Ma, Xiaoyan,Tian, Chao,Shi, Xueqi,Zhu, Renzong,Cheng, Can,Du, Yansheng,Ma, Zhizhong,Zhang, Zhili,Liu, Junyi
, p. 4302 - 4312 (2014/06/09)
Novel (E)-3,4-dihydroxystyryl aralkyl sulfones and sulfoxides were designed and synthesized as new analogues of 1, which showed interesting multifunctional neuroprotective effects, including antioxidative and antineuroinflammatory properties. Specifically, target compounds display excellent potency in scavenging reactive free radicals and demonstrate potent effects against various kinds of toxicities, including H2O2, 6-hydroxydopamine, and lipopolysaccharide in different types of neuronal cells. The antioxidative properties of the target compounds are more potent than that of 1, and the antineuroinflammatory properties are less strong than that of 1. According to the parallel artificial membrane permeation assay for the blood-brain barrier, target compounds possess greater blood-brain barrier (BBB) permeability than 1. In short, due to improvement of the antioxidative effect, stability, and BBB permeability, (E)-3,4-dihydroxystyryl aralkyl sulfones and sulfoxides can thus be considered as potential multifunctional neuroprotective agents and serve as new lead candidates in the treatment of neurodegenerative diseases.
