2-arylmethyl-1,4-benzoquinones .2. 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 rel...

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Bibliographic Details
Published inChemical & pharmaceutical bulletin Vol. 45; no. 4; pp. 668 - 674
Main Authors Suzuki, K, Tatsuoka, T, Ishihara, T, Ogino, R, Miyazaki, T, Satoh, F, Miyano, S, Sumoto, K
Format Journal Article
LanguageEnglish
Published TOKYO Pharmaceutical Soc Japan 01.04.1997
Subjects
Chemistry
Chemistry, Medicinal
Chemistry, Multidisciplinary
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Physical Sciences
Science & Technology
arachidonic acid
1,4-benzoquinone
anti-platelet aggregation
endothelial cell
hydrogen peroxide
PROSTAGLANDIN
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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 (A.A) with an IC50 in the range of 1-10 mu g/ml. Among them, 3b showed a significant inhibitory activity against endothelial cell injury caused by hydrogen peroxide (H2O2) at 1 mu m.
ISSN:0009-2363