Synthesis of Thiohydrouracils and Their Inhibitory Activity againstHill Reaction

Abstract

In order to find highly active inhibitors of Hill reaction, a series of thiohydrouracil derivatives have been synthesized by a four-step synthetic route. The structures of all compounds were confirmed by elemental analysis, ¹H NMR and IR spectra. Preliminary bioassay showed that these compounds could inhibit Hill reaction effectively, for example, compound 5j exhibited high inhibitory activity with IC₅₀＝0.82 g•mL^－1.

Key words: thiohydrouracil, Hill reaction, inhibition, synthesis

Cite this article

YAO Chang-Sheng,ZHU Ye-Rong²,HU Fang-Zhong,ZOU Xiao-Mao
ZHU You-Quan,GAO Ying,WANG Yong²,YANG Hua-Zheng*^,1. Synthesis of Thiohydrouracils and Their Inhibitory Activity againstHill Reaction[J]. Chin. J. Org. Chem., 2005, 25(07): 865-868.

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硫代氢化脲嘧啶的合成及其对Hill反应的抑制活性