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題名 | α-Methylene-γ-butyrolactones: Synthesis and Cardiovascular Evaluation of Flavone Derivatives |
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作者 | 趙越玲; 王泰吉; 陳義龍; 張雅玲; 鄧哲明; 曾誠齊; | 書刊名 | 中華藥學雜誌 |
卷期 | 51:1 1999.02[民88.02] |
頁次 | 頁49-63 |
分類號 | 414.7 |
關鍵詞 | 血小板凝集; α-Methylene-γ-butyrolactone; Flavone; Reformatsky-type condensation; Antiplatelet; |
語文 | 英文(English) |
英文摘要 | In a search for inhibitors of platelet aggregation, a number of flavone derivatives with α-methylene-γ-butyrolactone substituted at C(3). and C(6)- positions were synthesized and evaluated for their antiplatelet activities against thrombin (Thr)-, arachidonic acid (AA)-, collagen (Col)-, and platelet-activating factor (PAP)-induced aggregation in washed rabbit platelets. These compounds were synthesized from 3-hydroxyflavone or 6-hydroxyflavone via alkylation and Reformatsky-type condensation. Certain 3-substituted derivatives (6a-c) showed moderate inhibitory activities against platelet aggregation induced by AA and PAP while others (6d-f) were inactive. Except for 7f, all the 6-substituted derivatives (7a-e) showed the same pharmacological profile with aspirin and inhibited only AA-induced aggregation. However, 7a-e were approximately thirty to one hundred times more potent than aspirin. |
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