中國醫藥大學機構典藏 China Medical University Repository, Taiwan:Item 310903500/924
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    题名: 1-苯甲基-2-(5-甲基-2-呋喃基)苯并咪唑類緣物之合成 及其抗血小板活性;Synthesis and Antiplatelet Activity of 1-Benzyl-2-(5-methyl-2-furyl)benzimidazole Analogs
    作者: 陳柏舟;Po-Chou Chen
    贡献者: 中國醫藥大學：藥物化學研究所碩士班
    关键词: 咪唑并[4,5-b]吡;啶;抗血小板;imidazo[4,5-b]pyridine;antiplatelet
    日期: 2007-07-09
    上传时间: 2009-08-13 09:37:20 (UTC+8)
    摘要: 本研究室於持續開發新型抗血小板凝集化合物過程中，合成了一個咪唑類衍生物1-苯甲基-2-(5-甲基-2-呋喃基)苯并咪唑(A)，並測試其抗血小板活性。結果顯示化合物A對於collagen、arachidonic acid、U46619所誘發之血小板凝集具有優越之抑制作用，具發展成為治療栓塞新藥之潛力。於是，本計畫以化合物A為先導化合物，設計其5-取代-1-取代苯基-2- (5-甲基-2-呋喃)苯并咪唑(1-17)及3-取代-2-(5-甲基-2-呋喃)咪唑[4,5-b]吡啶 (19-71)等兩類類緣物。
    本論文旨在從事上述標的化合物之合成及其抗血小板活性評估。部分標的化合物顯示和化合物A相同模式之活性，即對於collagen所引發的血小板凝集具有抑制作用。其研究結果將增加我們對於benzimidazole衍生物的結構與活性間關係的知識，也期待能找到具抗血小板活性的新化合物。

    As a result of our continuing study aimed at the discovery and development of novel antiplatelet agents, 1-benzyl-2-(5-methyl-2-furyl) benzimidazole (A) was synthesized and evaluated for its antiplatelet activity. The preliminary results of compound A showed good inbibitory effect on collagen, arachidonic acid, U46619-induced platelet aggregation, it can be developed as a new category of drug to treat thrombosis. Encourage by this results, compound A was selected as a lead compound in this article. Two target analogs of benzimidazole were designed, they are 5-substituted-1-substisutedbenzyl-2-(5-methyl-2-furyl) benzimidazole (1-17) and 3-substituted-2-(5-methyl-2-furyl)imidazo [4,5-b]pyridine (19-71).
    In this article, we aim at synthesizing and evaluating their antiplatelet activities. Some of the target compounds showed the same pattern as compound A and exhibit highly inhibitory activity against platelet aggregation induced by collagen. The finding will add to our understanding of SAR of benzimidazoles. The goal of our continuing studies is to identify novel compounds for antiplatelet study.
    显示于类别:[藥物化學研究所] 博碩士論文

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