Synthesis and antiplatelet effects of omega-aminoalkoxylxanthones.
A series of omega-aminoalkoxylxanthones were synthesized and tested in-vitro for their ability to inhibit aggregation of rabbit washed platelets and human platelet-rich plasma (PRP) induced by various inducers. Nine of these compounds showed more potent antiplatelet effects than natural norathyriol tetraacetate on collagen-induced aggregation. The various omega-aminoalkoxyl side chains of the synthesized compounds modified the antiplatelet effects. All the compounds tested in human PRP showed significant inhibition of secondary aggregation induced by adrenaline, suggesting that the antiplatelet effects of these compounds is mainly due to an inhibitory effect on thromboxane formation. These compounds at high concentration also cause vasorelaxing action in rat thoracic aorta.
Lin
C N
CN
School of Pharmacy, Kaohsuing Medical College, Taiwan, ROC.
Liou
S S
SS
Lai
S C
SC
Lin
H C
HC
Ko
F N
FN
Liu
H W
HW
Teng
C M
CM
D000818:Animals; D016718:Arachidonic Acid / Q000494:pharmacology; D003094:Collagen; D005260:Female; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D010972:Platelet Activating Factor / Q000494:pharmacology; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011817:Rabbits; D051381:Rats; D017208:Rats, Wistar; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship; D013917:Thrombin / Q000494:pharmacology; D014966:Xanthenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
D010972:Platelet Activating Factor; D010975:Platelet Aggregation Inhibitors; D014966:Xanthenes; D016718:Arachidonic Acid; D003094:Collagen; D013917:Thrombin