2-Arylmethyl-1, 4-benzoquinones. II. Novel Inhibitors of Platelet Aggregation : Synthesis and Pharmacological Evaluation

Two new series of 2-arylmethyl-1, 4-benzoquinones (2 and 3) were synthesized for evaluation of their pharmacological activities. These compounds showed significant inhibition of platelet aggregation and some of them possessed a protective effect against endothelial cell injury. Structure-activity re...

Full description

Saved in:
Bibliographic Details
Published inChemical & pharmaceutical bulletin Vol. 45; no. 4; pp. 668 - 674
Main Authors SUZUKI, Kenji, TATSUOKA, Toshio, ISHIHARA, Takafumi, OGINO, Ryoko, MIYAZAKI, Tomoko, SATOH, Fumio, MIYANO, Seiji, SUMOTO, Kunihiro
Format Journal Article
LanguageEnglish
Published Tokyo The Pharmaceutical Society of Japan 1997
Maruzen
Subjects
1, 4-benzoquinone
Animals
anti-platelet aggregation
arachidonic acid
Arachidonic Acid - pharmacology
Benzoquinones - chemistry
Benzoquinones - pharmacology
Biological and medical sciences
Blood. Blood coagulation. Reticuloendothelial system
endothelial cell
Endothelium, Vascular - drug effects
Endothelium, Vascular - metabolism
hydrogen peroxide
Hydrogen Peroxide - metabolism
Male
Medical sciences
Pharmacology. Drug treatments
Platelet Aggregation - drug effects
Platelet Aggregation Inhibitors - chemical synthesis
Rabbits
Structure-Activity Relationship
Endothelial cell
Enzyme
Quinone
Enzyme inhibitor
Rabbit
Anticoagulant
Lagomorpha
Oxygen heterocycle
Morpholine derivatives
In vitro
Antiplatelet agent
L-Lactate dehydrogenase
Vertebrata
Mammalia
Cytoprotector
Structure activity relation
Animal
Bicyclic compound
Carboxamide
Benzenic compound
Aromatic compound
Oxidoreductases
Benzofuran derivatives
Chemical synthesis
Online AccessGet full text

Cover

More Information
Summary:Two new series of 2-arylmethyl-1, 4-benzoquinones (2 and 3) were synthesized for evaluation of their pharmacological activities. These compounds showed significant inhibition of platelet aggregation and some of them possessed a protective effect against endothelial cell injury. Structure-activity relationship studies indicated that 2b, 2d and 3b are potent inhibitors of platelet aggregation induced by arachidonic acid (AA) with an IC50 in the range of 1-10 μg/ml. Among them, 3b showed a significant inhibitory activity against endothelial cell injury caused by hydrogen peroxide (H2O2) at 1 μM.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0009-2363
1347-5223
DOI:10.1248/cpb.45.668