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A novel kind of acetohydroxyacid synthase(AHAS) inhibitors, arylsulfonylaminocarbonyl-2-thiohydantoins, was synthesized based on biorational design. The structures of these compounds were confirmed by IR, MS, NMR, and elemental analysis. The results of the preliminary activity tests indicate that most of the arylsulfonylamidecarbonyl-5-methyl-2-thiohydantoins have a higher biological activity than those without 5-methyl substituent.