利用D-(—)-Quinic acid合成Polyhydroxylated 7-alkylazepanes 作為Glycosidase抑制劑

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Title:	利用D-(—)-Quinic acid合成Polyhydroxylated 7-alkylazepanes 作為Glycosidase抑制劑
Other Titles:	Synthesis of polyhydorxylated 7-alkylazepanes as potent glycosidase inhibitors from D-(-)-quinic acid.
Authors:	梁名琮;Liang, Ming-tsung
Contributors:	淡江大學化學學系碩士班施增廉;Shih, Tzenge-lien
Keywords:	醣水解酵素抑制劑;Polyhydroxylated 7-alkylazepanes;D-(—)-Quinic acid;Glycosidase inhibitors
Date:	2008
Issue Date:	2010-01-11 02:40:43 (UTC+8)
Abstract:	長期以來，化學家對polyhydroxylated piperidines與其衍生物作為醣水解酵素抑制劑 (glycosidase inhibitors) 的功用研究較為廣泛，因為其具有潛力發展成治療癌症、糖尿病、病毒感染的藥物。　　而早期研究發現，六圓環azasugars中具methyl官能基之分子，對醣水解酵素有相當好的抑劑效果。例如：Dexoxyfucon-ojirimycin (1,5-Dideoxy-1,5-imino-L-fucitol)，對α-fucosidase有相當好的抑制活性 (Ki = 0.0013μM)；本實驗室過去著重在七圓環含氮分子 (azepanes)的合成，因為有研究報導七圓環之azasugars (azepanes)較六圓環azasugars結構上更具彈性，更容易嵌入酵素的活化中心，進而達到更良好的抑制效果；而azepanes中具烷類取代基的分子至今尚未見諸於文獻報導。為了解以上推論之基礎，因此我們合成了一系列具立體化學特異性的polyhydroxylated 7-methyl-及7-butylazepanes，來探討azepanes 之C-7位置上具烷基的取代基對醣水解酵素活性是否有決定性影響。 The biological activities of polyhydroxylated piperidines and their derivatives have been extensively studied during the past decades. These molecules are potentially therapeutic agents, especially, to serve as glycosidase inhibitors in treatment of cancers, diabetes and viral infections. The C- and N-alkylated piperidines are competitive glycosidase inhibitors to their corresponding molecules. Among them, deoxyfuconojirimycin (1,5-deoxy-1,5-imino-L-fucitol) was inhibitor against
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