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

Pei Wen Hsieh; Tsong Long Hwang; Chin Chung Wu; Fang Rong Chang; Tsai Wei Wang; Yang Chang Wu

doi:10.1016/j.bmcl.2005.03.104

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

Pei Wen Hsieh, Tsong Long Hwang, Chin Chung Wu, Fang Rong Chang, Tsai Wei Wang, Yang Chang Wu^*

^*Corresponding author for this work

School of Traditional Chinese Medicine

Kaohsiung Medical University

Research output: Contribution to journal › Journal Article › peer-review

58 Scopus citations

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.

Original language	English
Pages (from-to)	2786-2789
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	15
Issue number	11
DOIs	https://doi.org/10.1016/j.bmcl.2005.03.104
State	Published - 02 06 2005

Keywords

Anti-platelet aggregation
Benzoxazinones
Neutrophil elastase
Superoxide generation

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10.1016/j.bmcl.2005.03.104

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

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.",

keywords = "Anti-platelet aggregation, Benzoxazinones, Neutrophil elastase, Superoxide generation",

author = "Hsieh, {Pei Wen} and Hwang, {Tsong Long} and Wu, {Chin Chung} and Chang, {Fang Rong} and Wang, {Tsai Wei} and Wu, {Yang Chang}",

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T1 - The evaluation of 2,8-disubstituted benzoxazinone derivatives as anti-inflammatory and anti-platelet aggregation agents

AU - Hsieh, Pei Wen

AU - Hwang, Tsong Long

AU - Wu, Chin Chung

AU - Chang, Fang Rong

AU - Wang, Tsai Wei

AU - Wu, Yang Chang

PY - 2005/6/2

Y1 - 2005/6/2

N2 - 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.

AB - 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.

KW - Anti-platelet aggregation

KW - Benzoxazinones

KW - Neutrophil elastase

KW - Superoxide generation

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M3 - 文章

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AN - SCOPUS:19544363236

SN - 0960-894X

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 11

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

Abstract

Keywords

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