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題名 | Antiplatelet Activity of 5-(2'-Alkoxycar-bonyl substituted phenoxy)furan-2-carboxylic Acid Derivatives=5-(2'-烷氧羰基具取代苯氧基)呋喃-2-羧酸衍生物之抗血小板活性 |
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作者 | 張嘉麟; 吳錦生; 鄧哲明; | 書刊名 | 中國醫藥科學雜誌 |
卷期 | 3:1 2002.03[民91.03] |
頁次 | 頁1-8 |
分類號 | 414.33 |
關鍵詞 | 5-(2'-烷氧羰基具取代苯氧基)呋喃-2-羧酸衍生物; 抗血小板活性; 5-(2'-Alkoxycarbonyl substituted phenoxy)furan-2-carboxylic acid derivatives; Antiplatelet activity; |
語文 | 英文(English) |
中文摘要 | 著者將一系列5-(2'-烷氧羰基具取代苯氧基)喃-2-羧酸(1b-12b)及其酯類(1a-12a)測試其分別以花生仁四烯酸(AA),膠原(collagen),血小板活化因子(PAF)及凝血酵素(thrombin)誘發的血小板凝集之抑制活性。發現酯類之抗血小板活性比羧酸類強,這可能與影響分子分配係數的極性有關,而與取代基之位置無關。它們的抗血小板活性均比阿斯匹靈(aspirin)弱,但對花生仁四烯酸誘發的血小板凝集之抑制活性最明顯,對凝血酵素誘發的血小板凝集之抑制活性最不明顯。然其真正的抗血小板活性機轉並不清楚。在這些化合物中,5-(2'-甲氧羰基-4'-溴苯氧基)�P喃-2-羧酸乙基酯(11a)具有較強的抗血小板活性。 |
英文摘要 | A series of 5-(2'-alkoxycarbonyl substituted phenoxy)furan-2-carboxylic acids (1b-12b) and their esters (1a-12a) were evaluated for their antiplatelet activity using inhibitory tests induced by arachidonic acid (AA), collagen, platelet-activating factor (PAF), and thrombin, respectively. We found that the esters were more potent than those of carboxylic acids on the antiplatelet activity using inhibitory tests induced by selected inducers. The major difference may be related to the molecular polarity, which may influence the partition coefficient of a molecular. It would seem that inhibitory potency has nothing to do with the substitution position. Their inhibitory potency was weaker than that of aspirin and showed the greatest strength against AA-induced and the weakest strength against thrombin-induced platelet aggregation. However, the precise mechanism responsible for the antiplatelet activity of these compounds is not known. Among them, ethyl 5-(2'-methoxycarbonyl-4'-bromophenoxy)furan-2-carboxylate (11a) showed greater potency on the antiplatelet activity. |
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