1,2,4-Oxadiazolidin-3,5-diones and 1,3,5-triazin-2,4,6-triones as cytosolic phospholipase A₂α inhibitors

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• 作者：Ariamala Gopalsamy ; Hui Yang ; John W. Ellingboe ; John C. McKew ; Steve Tam ; Diane Joseph-McCarthy ; Wen Zhang ; Marina Shen and James D. Clark
• 关键词：1 ; 2 ; 4-Oxadiazolidin-3 ; 5-dione ; 1 ; 3 ; 5-Triazin-2 ; 4 ; 6-trione ; Cytosolic phospholipase A₂α ; inhibitors
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 出版时间：1 June 2006
• 年：2006
• 卷：16
• 期：11
• 页码：2978-2981
• 全文大小：181 K

文摘

1,2,4-Oxadiazolidin-3,5-dione and 1,3,5-triazin-2,4,6-trione scaffolds were employed as templates to incorporate the pharmacophore requirements of cytosolic phospholipase A₂α substrate mimetics. Inhibitors that are active in both enzyme, and cell-based assays were identified from both classes. From the SAR work carried out and modeling efforts around these templates, the triazinetrione scaffold with an additional substitution point was found to be more favorable.