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. 2007 Jun 1;15(11):3703-10.
doi: 10.1016/j.bmc.2007.03.045. Epub 2007 Mar 18.

Polyphenols based on isoflavones as inhibitors of Helicobacter pylori urease

Zhu-Ping Xiao  1 , Da-Hua Shi, Huan-Qiu Li, Li-Na Zhang, Chen Xu, Hai-Liang Zhu
Affiliations

Polyphenols based on isoflavones as inhibitors of Helicobacter pylori urease

Zhu-Ping Xiao et al. Bioorg Med Chem. .

Abstract

Twenty polyphenols were synthesized and evaluated for their effect on Helicobacter pylori urease. Among these compounds, 4-(p-hydroxyphenethyl)pyrogallol (15) (IC(50)=0.03 mM) and 7,8,4'-trihydroxyisoflavone (19) (IC(50)=0.14 mM) showed potent inhibitory activities, and inhibited Helicobacter pylori urease in a time-dependent manner. The structure-activity relationship of these polyphenols revealed: the two ortho hydroxyl groups were essential for inhibitory activity of polyphenol. When the C-ring of isoflavone was broken, the inhibitory activity markedly decreased. As for deoxybenzoin, the carboxyl group was clearly detrimental.

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