Medicinal Chemistry Research p. 403 - 412 (2010)
Update date:2022-08-03
Topics:
Zhang, Xue-Wu
Zhao, Dong-Hai
Quan, Ying-Chun
Sun, Liang-Peng
Yin, Xiu-Mei
Guan, Li-Ping
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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