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.
Hsieh
Pei-Wen
PW
Graduate Institute of Natural Products, Kaohsiung Medical University, Taiwan.
Hwang
Tsong-Long
TL
Wu
Chin-Chung
CC
Chang
Fang-Rong
FR
Wang
Tsai-Wei
TW
Wu
Yang-Chang
YC
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D048588:Benzoxazines / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D048588:Benzoxazines; D010975:Platelet Aggregation Inhibitors