The evaluation and structure-activity relationships of 2-benzoylaminobenzoic esters and their analogues as anti-inflammatory and anti-platelet aggregation agents

Pei Wen Hsieh; Tsong Long Hwang; Chin Chung Wu; Shin Zan Chiang; Chung I. Wu; Yang Chang Wu

doi:10.1016/j.bmcl.2006.12.038

The evaluation and structure-activity relationships of 2-benzoylaminobenzoic esters and their analogues as anti-inflammatory and anti-platelet aggregation agents

Pei Wen Hsieh, Tsong Long Hwang, Chin Chung Wu, Shin Zan Chiang, Chung I. Wu, 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

19 Scopus citations

Abstract

Forty-seven 2-benzoylaminobenzoic esters were synthesized and evaluated in anti-platelet aggregation, inhibition of superoxide anion generation, and inhibition of neutrophil elastase release assays. Most 2-benzoylamino-4-chlorobenzoic acid derivatives showed selective inhibitory effects on arachidonic acid (AA)-induced platelet aggregation. Among them, compounds 6b and 7b exhibited more potent inhibitory effects (ca. 200-fold) than aspirin. Additionally, compounds 1a and 5a showed strong inhibitory effects on neutrophil superoxide generation with IC₅₀ values of 0.65 and 0.17 μM, respectively. However, compounds 6d and 6e exhibited dual inhibitory effects on platelet aggregation and neutrophil elastase (NE) release; therefore, these two compounds may be new leads for development as anti-inflammatory and anti-platelet aggregatory agents.

Original language	English
Pages (from-to)	1812-1817
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	17
Issue number	6
DOIs	https://doi.org/10.1016/j.bmcl.2006.12.038
State	Published - 15 03 2007

Keywords

2-Benzoylaminobenzoic esters
Anti-inflammatory
Anti-platelet aggregation agents

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10.1016/j.bmcl.2006.12.038

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title = "The evaluation and structure-activity relationships of 2-benzoylaminobenzoic esters and their analogues as anti-inflammatory and anti-platelet aggregation agents",

abstract = "Forty-seven 2-benzoylaminobenzoic esters were synthesized and evaluated in anti-platelet aggregation, inhibition of superoxide anion generation, and inhibition of neutrophil elastase release assays. Most 2-benzoylamino-4-chlorobenzoic acid derivatives showed selective inhibitory effects on arachidonic acid (AA)-induced platelet aggregation. Among them, compounds 6b and 7b exhibited more potent inhibitory effects (ca. 200-fold) than aspirin. Additionally, compounds 1a and 5a showed strong inhibitory effects on neutrophil superoxide generation with IC50 values of 0.65 and 0.17 μM, respectively. However, compounds 6d and 6e exhibited dual inhibitory effects on platelet aggregation and neutrophil elastase (NE) release; therefore, these two compounds may be new leads for development as anti-inflammatory and anti-platelet aggregatory agents.",

keywords = "2-Benzoylaminobenzoic esters, Anti-inflammatory, Anti-platelet aggregation agents",

author = "Hsieh, {Pei Wen} and Hwang, {Tsong Long} and Wu, {Chin Chung} and Chiang, {Shin Zan} and Wu, {Chung I.} and Wu, {Yang Chang}",

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volume = "17",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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The evaluation and structure-activity relationships of 2-benzoylaminobenzoic esters and their analogues as anti-inflammatory and anti-platelet aggregation agents. / Hsieh, Pei Wen ; Hwang, Tsong Long; Wu, Chin Chung et al.
In: Bioorganic and Medicinal Chemistry Letters, Vol. 17, No. 6, 15.03.2007, p. 1812-1817.

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

TY - JOUR

T1 - The evaluation and structure-activity relationships of 2-benzoylaminobenzoic esters and their analogues as anti-inflammatory and anti-platelet aggregation agents

AU - Hsieh, Pei Wen

AU - Hwang, Tsong Long

AU - Wu, Chin Chung

AU - Chiang, Shin Zan

AU - Wu, Chung I.

AU - Wu, Yang Chang

PY - 2007/3/15

Y1 - 2007/3/15

N2 - Forty-seven 2-benzoylaminobenzoic esters were synthesized and evaluated in anti-platelet aggregation, inhibition of superoxide anion generation, and inhibition of neutrophil elastase release assays. Most 2-benzoylamino-4-chlorobenzoic acid derivatives showed selective inhibitory effects on arachidonic acid (AA)-induced platelet aggregation. Among them, compounds 6b and 7b exhibited more potent inhibitory effects (ca. 200-fold) than aspirin. Additionally, compounds 1a and 5a showed strong inhibitory effects on neutrophil superoxide generation with IC50 values of 0.65 and 0.17 μM, respectively. However, compounds 6d and 6e exhibited dual inhibitory effects on platelet aggregation and neutrophil elastase (NE) release; therefore, these two compounds may be new leads for development as anti-inflammatory and anti-platelet aggregatory agents.

AB - Forty-seven 2-benzoylaminobenzoic esters were synthesized and evaluated in anti-platelet aggregation, inhibition of superoxide anion generation, and inhibition of neutrophil elastase release assays. Most 2-benzoylamino-4-chlorobenzoic acid derivatives showed selective inhibitory effects on arachidonic acid (AA)-induced platelet aggregation. Among them, compounds 6b and 7b exhibited more potent inhibitory effects (ca. 200-fold) than aspirin. Additionally, compounds 1a and 5a showed strong inhibitory effects on neutrophil superoxide generation with IC50 values of 0.65 and 0.17 μM, respectively. However, compounds 6d and 6e exhibited dual inhibitory effects on platelet aggregation and neutrophil elastase (NE) release; therefore, these two compounds may be new leads for development as anti-inflammatory and anti-platelet aggregatory agents.

KW - 2-Benzoylaminobenzoic esters

KW - Anti-inflammatory

KW - Anti-platelet aggregation agents

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SN - 0960-894X

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 6

ER -

The evaluation and structure-activity relationships of 2-benzoylaminobenzoic esters and their analogues as anti-inflammatory and anti-platelet aggregation agents

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Keywords

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