Synthesis and anti-platelet evaluation of 2-benzoylaminobenzoate analogs

Pei Wen Hsieh; Shin Zan Chiang; Chin Chung Wu; Yi Ching Lo; Yu Tzu Shih; Yang Chang Wu

doi:10.1016/j.bmc.2008.03.071

Synthesis and anti-platelet evaluation of 2-benzoylaminobenzoate analogs

Pei Wen Hsieh^*
, Shin Zan Chiang
, Chin Chung Wu
, Yi Ching Lo
, Yu Tzu Shih
, Yang Chang Wu

^*Corresponding author for this work

Kaohsiung Medical University

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

8 Scopus citations

Abstract

Fifty-two 2-benzoylaminobenzoate analogs were synthesized and subjected to anti-platelet aggregation assay using arachidonic acid (AA), collagen (Col), thrombin (Thr), and U46619 as inducers. The results revealed that most of 2-benzoylaminobenzoic acid derivatives showed a selectively inhibitory effect on AA-induced platelet aggregation. As a result of the 2-benzoylaminobenzoic acid derivatives (18, 44, and 46), there were no inhibitory effects on platelet aggregation induced by U46619, but these elicited an inhibitory effect on thromboxane B₂ formation at 1.0 μM. These 2-benzoylaminobenzoate analogs were therefore proposed as cyclooxygenase inhibitors.

Original language	English
Pages (from-to)	5803-5814
Number of pages	12
Journal	Bioorganic and Medicinal Chemistry
Volume	16
Issue number	10
DOIs	https://doi.org/10.1016/j.bmc.2008.03.071
State	Published - 15 05 2008
Externally published	Yes

Keywords

2-Benzoylaminobenzoate analogs
Anti-platelet aggregation
Cyclooxygenase
Structure-activity relationships (SAR)

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.bmc.2008.03.071

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title = "Synthesis and anti-platelet evaluation of 2-benzoylaminobenzoate analogs",

abstract = "Fifty-two 2-benzoylaminobenzoate analogs were synthesized and subjected to anti-platelet aggregation assay using arachidonic acid (AA), collagen (Col), thrombin (Thr), and U46619 as inducers. The results revealed that most of 2-benzoylaminobenzoic acid derivatives showed a selectively inhibitory effect on AA-induced platelet aggregation. As a result of the 2-benzoylaminobenzoic acid derivatives (18, 44, and 46), there were no inhibitory effects on platelet aggregation induced by U46619, but these elicited an inhibitory effect on thromboxane B2 formation at 1.0 μM. These 2-benzoylaminobenzoate analogs were therefore proposed as cyclooxygenase inhibitors.",

keywords = "2-Benzoylaminobenzoate analogs, Anti-platelet aggregation, Cyclooxygenase, Structure-activity relationships (SAR)",

author = "Hsieh, \{Pei Wen\} and Chiang, \{Shin Zan\} and Wu, \{Chin Chung\} and Lo, \{Yi Ching\} and Shih, \{Yu Tzu\} and Wu, \{Yang Chang\}",

year = "2008",

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day = "15",

doi = "10.1016/j.bmc.2008.03.071",

language = "英语",

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pages = "5803--5814",

journal = "Bioorganic and Medicinal Chemistry",

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}

TY - JOUR

T1 - Synthesis and anti-platelet evaluation of 2-benzoylaminobenzoate analogs

AU - Hsieh, Pei Wen

AU - Chiang, Shin Zan

AU - Wu, Chin Chung

AU - Lo, Yi Ching

AU - Shih, Yu Tzu

AU - Wu, Yang Chang

PY - 2008/5/15

Y1 - 2008/5/15

N2 - Fifty-two 2-benzoylaminobenzoate analogs were synthesized and subjected to anti-platelet aggregation assay using arachidonic acid (AA), collagen (Col), thrombin (Thr), and U46619 as inducers. The results revealed that most of 2-benzoylaminobenzoic acid derivatives showed a selectively inhibitory effect on AA-induced platelet aggregation. As a result of the 2-benzoylaminobenzoic acid derivatives (18, 44, and 46), there were no inhibitory effects on platelet aggregation induced by U46619, but these elicited an inhibitory effect on thromboxane B2 formation at 1.0 μM. These 2-benzoylaminobenzoate analogs were therefore proposed as cyclooxygenase inhibitors.

AB - Fifty-two 2-benzoylaminobenzoate analogs were synthesized and subjected to anti-platelet aggregation assay using arachidonic acid (AA), collagen (Col), thrombin (Thr), and U46619 as inducers. The results revealed that most of 2-benzoylaminobenzoic acid derivatives showed a selectively inhibitory effect on AA-induced platelet aggregation. As a result of the 2-benzoylaminobenzoic acid derivatives (18, 44, and 46), there were no inhibitory effects on platelet aggregation induced by U46619, but these elicited an inhibitory effect on thromboxane B2 formation at 1.0 μM. These 2-benzoylaminobenzoate analogs were therefore proposed as cyclooxygenase inhibitors.

KW - 2-Benzoylaminobenzoate analogs

KW - Anti-platelet aggregation

KW - Cyclooxygenase

KW - Structure-activity relationships (SAR)

UR - https://www.scopus.com/pages/publications/43749084144

U2 - 10.1016/j.bmc.2008.03.071

DO - 10.1016/j.bmc.2008.03.071

M3 - 文章

C2 - 18407506

AN - SCOPUS:43749084144

SN - 0968-0896

VL - 16

SP - 5803

EP - 5814

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 10

ER -

Synthesis and anti-platelet evaluation of 2-benzoylaminobenzoate analogs

Abstract

Keywords

UN SDGs

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