合成（5 -甲基-2-?喃基）咪唑[4,5-b]?啶衍生物作為抗血小板藥物

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題名:	合成（5 -甲基-2-?喃基）咪唑[4,5-b]?啶衍生物作為抗血小板藥物 Synthesis of (5-methyl-2-furyl) imidazo [4,5-b]pyridine Derivatives as Antiplatelet Agents
作者:	楊君鼎;Yang, Chun-Ting
貢獻者:	藥物化學研究所碩士班
關鍵詞:	（5 -甲基-2-?喃基）;咪唑[4,5-b]?啶;(5-methyl-2-furyl);imidazo [4,5-b]pyridine
日期:	2012-08-30
上傳時間:	2012-09-25 14:14:01 (UTC+8)
出版者:	中國醫藥大學
摘要:	在持續研發新型抗血小板凝集的藥物過程中，合成1-benzyl-2-(5-methyl-2-furyl)benzimidazole ( I )並測試其抗血小板活性，結果顯示化合物 I 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 I 為先導化合物，設計並合成 5(或 6)-鹵素-1-取代苯甲基-2-（5-甲基-2 -呋喃）咪唑并[4,5-b]吡啶一系列化合物，再經管柱層析分離後，得到的化合物 3~40 進行血小板評估。本論文旨在從事上述標的化合物之合成及其抗血小板評估，部分標的化合物顯示和化合物 I 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，而化合物 30 亦對於 U46619 (10μM)所誘導之血小板凝集表現出良好抑制活性。此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。 In continuing development of novel aniplatelet agents, we had found that 1-benzyl-2-(5-methyl-2-furyl)benzimidazole ( I ) showed good platelet inhibitory activity. Compound I showed good inhibitory effect on the platelet aggregation induced by collagen、arachidonic acid、U46619. Encouraged by this result,the Compound I was selected as a lead compound and a series of 5(or 6)-halo-1-substituted benzyl-2-(5-methyl-2-furyl)imidazo[4,5-b]pyridine (3~40) were synthesized in this work. All the synthesized compounds were evaluated for their antiplatelet activities. In this article, we aim at synthesizing and evaluating their antiplatelet activities. Some of the target compounds showed the same pattern as compound I and exhibited highly inhibitory activity against platelet aggregation induced by collagen. Compound 30 also showed good inhibitory effects on platelet aggregation induced by U46619(10μM). The finding will add to our understanding of SAR of benzimidazoles. The gole of our continuing studies is to identify novel compounds for antiplatelet study.
顯示於類別:	[藥物化學研究所] 博碩士論文

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