1-取代 2-(5'-甲基-2'-■喃基)苯駢咪■的合成及其抗血小板活性; Synthesis and Antiplatelet Activity of 1-Substituted 2-(5'-methyl-2'-furyl)benzimidazoles

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Title:	1-取代 2-(5'-甲基-2'-■喃基)苯駢咪■的合成及其抗血小板活性;Synthesis and Antiplatelet Activity of 1-Substituted 2-(5'-methyl-2'-furyl)benzimidazoles
Authors:	謝英雪;Hsieh, Ying-hsueh
Contributors:	中國醫藥學院藥物化學研究所
Date:	1999
Issue Date:	2009-12-02 14:20:21 (UTC+8)
Abstract:	為了更進一步了解YC-1類緣化合物的構效關係(SAR)，著者選擇了5-甲基-■喃甲醛(5-methyl furfuryl)(2)為起始原料，在醋酸銅的存在下和對-苯二胺(o-phenyldiamine)(1)進行縮合反應，而得到2-(5'-甲基-2'-■喃基)苯駢咪■(3)，緊接著和有取代的芐基氯(benzyl chlorides)反應，即可得到1-取代2-(5'-甲基-2'-■喃基)苯駢咪■(4~6)等標的化合物。 3和4已測其抗血小板活性，此二個化合物對花生四烯酸和膠原所誘導的血小板凝集具有明顯的抑制作用，其IC50值分別為12.2、32.4μg/ml及7.5、20.9μg/ml。; To further explore the structure-activity relationship of YC-1 analogs in this work, I selected 5-methyl furfural (2) as starting material for condensation with o-phenyldiamine (1), in the precence of cupric acetate, to afford 2-(5´-methyl-2´-furyl) benzimidazole (3). Compound 3 was subsequently reacted with substituted benzyl chlorides to yield the 1-substituted benzl-2- (5´-methyl-2´-furyl)benzimidazoles (4~6). The antiplatelet activity of target compounds 3 and 4 were examined. Both compounds exhibit significant inhibitory effect against AA and collagen-induced platelet aggregation with IC50 values of 12.2μg/ml、32.4μg/ml，7.5μg/ml、20.9μg/ml respectively.
Appears in Collections:	[Graduate Institute of Pharmaceutical Chemistry] Theses & dissertations

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