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Bioorg Med Chem Lett ; 21(5): 1549-53, 2011 Mar 01.
Article in English | MEDLINE | ID: mdl-21288716

ABSTRACT

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.


Subject(s)
Acrylates/chemical synthesis , Anti-Inflammatory Agents/chemical synthesis , Drug Design , Phenol/chemical synthesis , Acrylates/chemistry , Acrylates/pharmacology , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/pharmacology , Coumaric Acids/chemistry , Molecular Structure , Phenol/chemistry , Phenol/pharmacology
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