The evaluation of 2,8-disubstituted benzoxazinone derivatives as anti-inflammatory and anti-platelet aggregation agents |
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Authors: | Hsieh Pei-Wen Hwang Tsong-Long Wu Chin-Chung Chang Fang-Rong Wang Tsai-Wei Wu Yang-Chang |
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Institution: | Graduate Institute of Natural Products, Kaohsiung Medical University, Taiwan. |
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Abstract: | 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. |
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