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α-1,3-半乳糖基转移酶选择性抑制剂的简明合成。

Concise syntheses of selective inhibitors against α-1,3-galactosyltransferase.

机构信息

State Key Laboratory of Natural and Biomimetic Drugs, Peking University, and School of Pharmaceutical Sciences, Peking University, Xue Yuan Road #38, Beijing 100191, China.

出版信息

Org Biomol Chem. 2010 Nov 21;8(22):5062-8. doi: 10.1039/c0ob00042f. Epub 2010 Sep 1.

Abstract

Several iminosugar-based uridine diphosphate galactose (UDP-Gal) mimetics 1-4 including d- and l-epimers were designed and synthesized by concise routes, and these synthetic compounds were evaluated for the inhibition of α-1,3- and β-1,4-galactosyltransferases in vitro. The experimental data demonstrated that l-epimer 2 displayed the strongest inhibitory activity with moderate selectivity against α-1,3-galactosyltransferase.

摘要

几种基于亚氨基糖的尿苷二磷酸半乳糖(UDP-Gal)类似物 1-4,包括 d-和 l-差向异构体,通过简洁的路线设计和合成,并对这些合成化合物进行了体外抑制 α-1,3-和 β-1,4-半乳糖基转移酶的活性评价。实验数据表明,l-差向异构体 2 对 α-1,3-半乳糖基转移酶具有最强的抑制活性和中等选择性。

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