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 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 micrograms/ml. Among them, 3b showed a significant inhibitory activity against endothelial cell injury caused by hydrogen peroxide (H2O2) at 1 microM.
Suzuki
K
K
Suntory Institute for Biomedical Research, Osaka, Japan.
Tatsuoka
T
T
Ishihara
T
T
Ogino
R
R
Miyazaki
T
T
Satoh
F
F
Miyano
S
S
Sumoto
K
K
D000818:Animals; D016718:Arachidonic Acid / Q000494:pharmacology; D016227:Benzoquinones / Q000737:chemistry* / Q000494:pharmacology; D004730:Endothelium, Vascular / Q000187:drug effects / Q000378:metabolism; D006861:Hydrogen Peroxide / Q000378:metabolism; D008297:Male; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis*; D011817:Rabbits; D013329:Structure-Activity Relationship
D016227:Benzoquinones; D010975:Platelet Aggregation Inhibitors; D016718:Arachidonic Acid; D006861:Hydrogen Peroxide