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

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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Sogawa S,Nihro Y,Ueda H,Izumi A,Miki T,Matsumoto H,Satoh T

doi

10.1021/jm00076a019

subject

Has Abstract

pub_date

1993-11-26 00:00:00

pages

3904-9

issue

24

eissn

0022-2623

issn

1520-4804

journal_volume

36

pub_type

杂志文章

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