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目的:研究一系列依布硒啉衍生物对白三烯 B4 生物合成的影响,并探讨其构效关系。方法:高效液相色谱法测定白三烯 B4 。结果:依布硒啉的磺酰胺类似物以及 N芳香环取代的磺酰胺衍生物对白三烯 B4 生物合成具有抑制作用,其 I C5 0 在10 - 5 ~10 - 6 mol· L- 1 之间,并存在一定的构效关系。结论:磺酰胺基团上的酸性氢原子是关键因素,它的存在可以形成分子内氢键,从而使化合物具有活性。
Objective: To study the effects of a series of ebselen derivatives on the biosynthesis of leukotriene B4 and its structure-activity relationship. Method: Determination of leukotriene B4 by high performance liquid chromatography. Results: The sulfonamide analogues of ebselen and N-aromatic ring-substituted sulfonamide derivatives have inhibitory effects on the biosynthesis of leukotriene B4. The I C5 0 is between 10 -5 and 10 -6 mol · L -1 There is a certain structure-activity relationship between them. Conclusion: The acidic hydrogen atom on the sulfonamide group is the key factor, and its existence can form an intramolecular hydrogen bond to make the compound active.