Antinociceptive properties of caffeic acid derivatives in mice

Ten ester derivatives from caffeic acid were synthesized, and their antinociceptive properties are evaluated in mice. The most active compound, dodecyl ester derivative, exhibited potent and dose-related activity against the writhing test, with a calculated ID 50 value of 15.1 (11.9–19.1) μmol/kg and MI of 78.8% being several times more active than reference drugs. It was also effective in other experimental models, such as formalin, capsaicin and glutamate-induced pain tests, but was inactive in the hot-plate test. Although the mechanism of action has still not been elucidated, these results appear to support its therapeutic potential against painful diseases. [Display omitted] Caffeic acid derivatives have been synthesized and tested for their antinociceptive activity in different models of pain and compared with some drugs used clinically. Some structural aspects are also discussed.