Two series of ω-phenoxy contained acylhydroxamic acids as novel urease inhibitors were designed and synthesized. Biological activity evaluations revealed that ω-phenoxypropinoylhydroxamic acids were more active than phenoxyacetohydroxamic acids. Out of these compounds, 3-(3,4-dichlorophenoxy)propionylhydroxamic acid c24 showed significant potency against urease in both cell free extract (IC₅₀ = 0.061 ± 0.003 μM) and intact cell (IC₅₀ = 0.89 ± 0.05 μM), being over 450- and 120-fold more potent than the clinically prescribed urease inhibitor AHA, repectively. Non-linear fitting of experimental data (V-[S]) suggested a mixed-type inhibition mechanism and a dual site binding mode of these compounds.

设计并合成了两个系列的ω-苯氧基含酰基异羟肟酸作为新型脲酶抑制剂。生物活性评估表明，ω-苯氧基丙酰基异羟肟酸比苯氧基乙氧基异羟肟酸更具活性。在这些化合物中，3-（3,4-二氯苯氧基）丙酰基异羟肟酸c24在无细胞提取物（IC ₅₀  = 0.061± 0.003μM）和完整细胞（IC ₅₀  = 0.89±0.05μM）中均表现出显着的抗脲酶活性。分别比临床规定的脲酶抑制剂AHA强450倍和120倍以上。实验数据的非线性拟合（V- [S]）表明了这些化合物的混合型抑制机制和双位点结合模式。