Synthesis and inhibitory activities on platelet aggregation of some flavonoid analogues.
A series of 26 benzodioxan and benzodioxol derivatives of flavone have been prepared. The activity of the compounds on washed human platelet aggregation induced by adenosine diphosphate (ADP, 5 mumol/l), collagen (10 micrograms/ml) and calcimycin (20 mumol/l) was evaluated. The alkoxycarbonyl side chain derivatives inhibited all three types of aggregation inducers. Among the tested compounds Ia is the most potent inhibitor of collagen-induced aggregation but possesses a weak activity against the other two used inducers. The esters IIIb and in particular, IIIc are active against all the three used inducers. These results suggest that ethoxycarbonyl group is a potent substituent to provide the antiplatelet action in this series of flavonoids.
Göker
H
H
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Ankara, Turkey.
Tunçbilek
M
M
Leoncini
G
G
Buzzi
E
E
Mazzei
M
M
Rolland
Y
Y
Ertan
R
R
D005419:Flavonoids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D005419:Flavonoids; D010975:Platelet Aggregation Inhibitors