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J Med Chem. 1993 Nov 26;36(24):3904-9.

3,4-Dihydroxychalcones as potent 5-lipoxygenase and cyclooxygenase inhibitors.

Author information

1
Faculty of Pharmaceutical Science, Tokushima Bunri University, Japan.

Abstract

A novel series of 3,4-dihydroxychalcones was synthesized to evaluate their effects against 5-lipoxygenase and cyclooxygenase. Almost all compounds exhibited potent inhibitory effects on 5-lipoxygenase with antioxidative effects, and some also inhibited cyclooxygenase. The 2',5'-disubstituted 3,4-dihydroxychalcones with hydroxy or alkoxy groups exhibited optimal inhibition of cyclooxygenase. We found that 2',5'-dimethoxy-3,4-dihydroxychalcone (37; HX-0836) inhibited cyclooxygenase to the same degree as flufenamic acid and 5-lipoxygenase, more than quercetin. Finally, these active inhibitors of 5-lipoxygenase inhibited arachidonic acid-induced mouse ear edema more than phenidone.

PMID:
8254620
DOI:
10.1021/jm00076a019
[Indexed for MEDLINE]

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