Abstract
In an effort to develop potent antiinflammatory agents, a series of substituted chalcone derivatives was synthesized and evaluated for antiinflammatory activity through monitoring of their ability to inhibit xylene-induced ear edema in mice. Some of the tested compounds exhibited significant activity, and compounds 3f [(E)-1-(2,4-dihydroxyphenyl)-3-(4-dimethylamino)phenyl)prop-2-en-1-one] and 3h [(E)-3-(4-chlorophenyl)-1-(2,4-dihydroxyphenyl)prop-2-en-1-one] showed the highest antiinflammatory activity (62 and 68% inhibition, respectively, 2 h before administration), comparable with or even slightly more potent than the reference drug ibuprofen (53%). Furthermore, the structure–activity relationship of these substituted chalcone derivatives was demonstrated.
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Zhang, XW., Zhao, DH., Quan, YC. et al. Synthesis and evaluation of antiinflammatory activity of substituted chalcone derivatives. Med Chem Res 19, 403–412 (2010). https://doi.org/10.1007/s00044-009-9202-z
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DOI: https://doi.org/10.1007/s00044-009-9202-z