Göker H, Tunçbilek M, Leoncini G, Buzzi E, Mazzei M, Rolland Y, Ertan R
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Ankara, Turkey.
Arzneimittelforschung. 1995 Feb;45(2):150-5.
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.
已制备了一系列26种黄酮的苯并二恶烷和苯并二恶唑衍生物。评估了这些化合物对由二磷酸腺苷（ADP，5 μmol/l）、胶原蛋白（10 μg/ml）和离子霉素（20 μmol/l）诱导的洗涤过的人血小板聚集的活性。烷氧羰基侧链衍生物抑制所有三种类型的聚集诱导剂。在所测试的化合物中，Ia是胶原蛋白诱导聚集的最有效抑制剂，但对其他两种所用诱导剂的活性较弱。酯IIIb，特别是IIIc对所有三种所用诱导剂均有活性。这些结果表明，乙氧羰基是在这一系列黄酮类化合物中提供抗血小板作用的有效取代基。
