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

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.

Graphical abstractNovel scaffolds based on 1,2,4-oxadiazolidin-3,5-dione and 1,3,5-triazin-2,4,6-trione are described as cytosolic phospholipase A2α substrate mimetics.Figure optionsDownload full-size imageDownload as PowerPoint slide