Synthesis, structure–activity relationship analysis and kinetics study of reductive derivatives of flavonoids as Helicobacter pylori urease inhibitors

…, ZY Peng, JJ Dong, J He, H Ouyang, YT Feng…

Index: Xiao, Zhu-Ping; Peng, Zhi-Yun; Dong, Jing-Jun; He, Juan; Ouyang, Hui; Feng, Yu-Ting; Lu, Chun-Lei; Lin, Wan-Qiang; Wang, Jin-Xiang; Xiang, Yin-Ping; Zhu, Hai-Liang European Journal of Medicinal Chemistry, 2013 , vol. 63, p. 685 - 695

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Citation Number: 20

Abstract

In a continuing study for discovering urease inhibitors based on flavonoids, nineteen reductive derivatives of flavonoids were synthesized and evaluated against Helicobacter pylori urease. Analysis of structure–activity relationship disclosed that 4-deoxy analogues are more potent than other reductive products. Out of them, 4′, 7, 8-trihydroxyl-2-isoflavene (13) was found to be the most active with IC50 of 0.85 μM, being over 20-fold more potent ...