頁籤選單縮合
題名 | Synthesis and Antiplatelet Activity of 3,5,6,7,8,2',3' and 4'-Disubstituted 2-Phenyl-4-Quinolones= |
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作者 | 謝明杰; 黃麗嬌; 吳天賞; 李國雄; 鄧哲明; 郭盛助; Hsieh, Ming-chieh; Huang, Li-jiau; Wu, Tian-shung; Lee, Kuo-hsiung; Teng, Che-ming; Kuo, Sheng-chu; |
期刊 | 中華藥學雜誌 |
出版日期 | 19981000 |
卷期 | 50:5 1998.10[民87.10] |
頁次 | 頁277-288 |
分類號 | 418.4 |
語文 | eng |
關鍵詞 | 2-phenyl-4-quinolone; Synthesis; Antiplatelet activity; Structure-activity relationships; |
英文摘要 | To further define the structure-activity relationships (SAR) of 2-phenyl-4-quinolone derivatives, a series of disubstituted derivatives were synthesized and their inhibitory effects against arachidonic acid (AA)-induced platelet aggregation were evaluated. The test results did not lead to a definitive SAR but will be used as a guideline for further development of quantitative structure-activity relationship studies. Some of the tested compounds did show significant antiplatelet activity. Among them, 5,7-dimethyl-2-phenyl-4-quinolone (32) exhibited the highest activity (IC�t=1.03 μ mol) with about 20 times the potency of aspirin, and was hence chosen as a new lead compound for further structural modification. |
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