29048-57-5Relevant academic research and scientific papers
Novel paeonol derivatives: Design, synthesis and anti-inflammatory activity in vitro and in vivo
Hu, Yang Sheng,Han, Xu,Yu, Pei Jing,Jiao, Ming Ming,Liu, Xin Hua,Shi, Jing Bo
, (2020/03/13)
Paeonol has been proved to have potential anti-inflammatory activity, but its clinical application is not extensive due to the poor anti-inflammatory activity (14.74% inhibitory activity at 20 μM). In order to discover novel lead compound with high anti-inflammatory activity, series of paeonol derivatives were designed and synthesized, their anti-inflammatory activities were screened in vitro and in vivo. Structure-activity relationships (SARs) have been fully concluded, and finally (E)-N-(4-(2-acetyl-5-methoxyphenoxy)phenyl)-3-(3,4,5-trimet-hoxyphenyl)acrylamide (compound 11a) was found to be the best active compound with low toxicity, which showed 96.32% inhibitory activity at 20 μM and IC50 value of 6.96 μM against LPS-induced over expression of nitric oxide (NO) in RAW 264.7 macrophages. Preliminary mechanism studies indicated that it could inhibit the expression of TLR4, resulting in inhibiting of NF-κB and MAPK pathways. Further studies have shown that compound 11a has obvious therapeutic effect against the adjuvant-induced rat arthritis model.
Paeonol acetic acid compound as well as preparation method and medicinal purpose thereof
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Paragraph 0121; 0122, (2017/10/26)
The invention relates to the field of pharmaceutical chemistry and pharmacotherapeutics, and particularly relates to a paeonol acetic acid compound as well as a preparation method and application thereof to pharmacy. The compound has an effect of platelet aggregation resistance, and can be used for preparing a medicine for treating cardiovascular and cerebrovascular diseases. The invention also relates to the preparation method of the compound.
