1-芐基-3-(5-取代-2-呋喃基)-5-甲氧基-1H-吲唑衍生物之合成、抗血小板、抗血管增生與細胞致毒活性; Synthesis，Antiplatelet，Antiangiogenesis and Cytotoxicity Activity of 1-Benzyl-3-(5-substituted-2-furyl)-5-methoxy-1H-indazole Derivatives

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题名:	1-芐基-3-(5-取代-2-呋喃基)-5-甲氧基-1H-吲唑衍生物之合成、抗血小板、抗血管增生與細胞致毒活性;Synthesis，Antiplatelet，Antiangiogenesis and Cytotoxicity Activity of 1-Benzyl-3-(5-substituted-2-furyl)-5-methoxy-1H-indazole Derivatives
作者:	蔡睿盈;Tsai, Ray-Ying
贡献者:	中國醫藥學院藥物化學研究所
关键词:	C型肝炎病毒;細胞因子;共同免疫沉澱法;非結構性蛋白質;抗血管增生;細胞致毒;YC-1;indazole;antiplatelet;antiangiogenesis;cytotoxicity
日期:	1992
上传时间:	2009-12-23
摘要:	中文摘要 1-芐基-3-(5'-羥甲基-2'-呋喃基)吲唑(YC-1)是本實驗室首次合成的一種新型抗血小板藥物，由於其生物活性特異且廣泛，因此，著者擬合成一系列YC-1之5-甲氧基衍生物並測試其生物活性。以甲基 5-(3-甲氧基苯醯基)-2-呋喃酯(1)為起始物質與芐基聯胺反應產生E-及Z-型異構物的混合物(2)。將此混合物於低溫下，與四醋酸鉛於二氯甲烷中進行反應後，再加入三氟化硼參與反應，進而加熱即可形成所預期的關鍵化合物甲基5-(1-芐基-5-甲氧基-1H-吲唑-3-基)-2-呋喃酯(4)。以甲基5-(1-芐基-5-甲氧基-1H-吲唑-3-基)-2-呋喃酯(4)作為合成酯類(8a—8d)、醯胺類(9a—9h)及胺基酸甲酯類(10a—10f)之起始物，所合成之化合物之藥理活性的篩選試驗仍在測試中。; Abstract 1-Benzyl-3-(5'-hydroxymethyl-2'-furyl)indazole (YC-1) was first synthesized in our laboratory as a novel antiplatelet agent. Encouraged by the initial results, a series of 5-methoxy derivatives of YC-1 analogues were synthesized and examined for their biological activities. The starting material methyl 5-(3-methoxybenzoyl)-2-furoate (1) was treated with benzylhydrazine to yield a mixture of E- and Z-form isomers 2. The hydrazone was then treated with lead tetraacetate in dichloromethane at low temperature, then boron trifluoride etherate was added and the mixture heated to form the expected key intermediate ：methyl 5-(1-benzyl-5-methoxy-1H-indazol-3-yl)-2-furoate (4). Starting from methyl 5-(1-benzyl-5-methoxy-1H-indazol-3-yl) -2-furoate (4), various esters 8a—8d、amides 9a—9h and amino acid methyl esters 10a—10f were synthesized，biological evaluation of the synthesized compounds are currently under investigation.
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