Synthesis, antiplatelet and vasorelaxing activities of xanthone derivatives.
A series of omega-aminoalkoxylxanthones was synthesized and tested in vitro for their ability to inhibit platelet aggregation and cause vasorelaxing action. Compounds 4, 5, 12, 17, and 18 showed significant antiplatelet effects on thrombin-, arachidonic acid (AA)-, collagen-, and platelet activating factor (PAF)-induced washed rabbit platelet aggregation and exhibited inhibition of primary and secondary aggregation induced by adenosine-5'-diphosphate (ADP) in human platelet-rich-plasma (PRP). Compounds 4, 17, and 18 revealed vasorelaxing activities in rat thoracic aorta. We concluded that these compounds may be developed as new antithrombotic agents.
Lin
Kai-Wei
KW
School of Pharmacy, Kaohsiung Medical University, Kaohsiung, Taiwan.
Fang
Song-Chwan
SC
Hung
Chi-Feng
CF
Shieh
Bor-Jinn
BJ
Yang
Shyh-Chyun
SC
Teng
Che-Ming
CM
Lin
Chun-Nan
CN
D000818:Animals; D001011:Aorta / Q000187:drug effects / Q000502:physiology; D002478:Cells, Cultured; D005343:Fibrinolytic Agents / Q000138:chemical synthesis*; D006801:Humans; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis*; D011817:Rabbits; D051381:Rats; D013329:Structure-Activity Relationship; D014664:Vasodilation / Q000187:drug effects; D014665:Vasodilator Agents / Q000138:chemical synthesis*; D044004:Xanthones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D005343:Fibrinolytic Agents; D010975:Platelet Aggregation Inhibitors; D014665:Vasodilator Agents; D044004:Xanthones