891149-35-2Relevant academic research and scientific papers
Design, synthesis and biological evaluation of novel 4-hydroxybenzene acrylic acid derivatives
Mao, Jin-Long,Ran, Xiang-Kai,Tian, Jing-Zhen,Jiao, Bo,Zhou, Hong-Lei,Chen, Li,Wang, Zhen-Guo
, p. 1549 - 1553 (2011/04/22)
A series of 4-hydroxybenzene acrylic acid derivatives were designed and synthesized based on the ferulic acid of natural active ingredients. The tested compound 5a, 5f and 6a have significant anti-inflammatory activity with suppression rates of 45.29%, 44.75% and 24.11%, respectively, compared with that of indomethacin, and their cardiac toxicity was not observed. The structure-function relationship shows that the p-hydroxyl group on the α-position benzene ring, particularly if acetylated, contributes to the considerable anti-inflammatory activity; that the carboxyl group on the double bond, if esterified, also contributes to the anti-inflammatory activity; that the p-methylsulfonyl group on the other benzene ring, whose introduction is due to the COX-2 selectivity, also contributes to anti-inflammatory activity surprisingly.
