The evaluation of 2,8-disubstituted benzoxazinone derivatives as anti-inflammatory and anti-platelet aggregation agents

A series of 2,8-disubstituted benzoxazinones were synthesized and subjected to anti-platelet aggregation, inhibition of superoxide anion generation, and inhibition of neutrophil elastase release assays. Among them, 2-(2′-substituted-phenyl)-benzoxazinones exhibited significant inhibitory effect to target assays. Additionally, all of them were more potent than aspirin on AA-induced platelet aggregation, and these suggested that 2-(2′-substituted-phenyl)-benzoxazinones also possess aspirin-like activity. On the other hand, the compounds 6 and 16 showed inhibitory effects on neutrophil elastase release and superoxide generation.

Graphical abstractA series of 2,8-disubstituted benzoxazinones were synthesized and subjected to anti-platelet aggregation, inhibition of superoxide anion generation, and inhibition of neutrophil elastase release assays. The results suggested that these compounds can provide the lead compounds for anti-inflammatory agents.Figure optionsDownload full-size imageDownload as PowerPoint slide