Structure–activity relationship on human serum paraoxonase (PON1) using substrate analogues and inhibitors

…, M Akhtar, K Biggadike, D Gani, RK Allemann

文献索引：Bargota, Rakesh S.; Akhtar, Mahmoud; Biggadike, Keith; Gani, David; Allemann, Rudolf K. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 10 p. 1623 - 1626

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被引用次数: 15

摘要

Substrate analogues based on the parent compounds paraoxon and phenyl acetate were tested on human serum paraoxonase (PON1) to explore the active site of the enzyme. Replacement of the nitro group of paraoxon with an amine or hydrogen, as well as electronic changes to the parent compound, converted these analogues into inhibitors. Introduction of either electron-withdrawing or donating groups onto phenyl acetate resulted in reduction ...