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...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Chemical & pharmaceutical bulletin 1997/04/15, Vol.45(4), pp.668-674
Hauptverfasser:	SUZUKI, Kenji, TATSUOKA, Toshio, ISHIHARA, Takafumi, OGINO, Ryoko, MIYAZAKI, Tomoko, SATOH, Fumio, MIYANO, Seiji, SUMOTO, Kunihiro
Format:	Artikel
Sprache:	eng
Schlagworte:	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
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	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.
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.45.668