Design, synthesis, and biological evaluation of human sialidase inhibitors. Part 1: Selective inhibitors of lysosomal sialidase (NEU1)
Design, synthesis, and biological evaluation of human sialidase inhibitors. Part 1: Selective inhibitors of lysosomal sialidase (NEU1)
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DOI：
10.1016/j.bmcl.2007.11.084
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发表时间：
2008-01-15
影响因子：
2.7
通讯作者：
Kiso, Makoto
中科院分区：
文献类型：
--
作者：
Magesh, Sadagopan;Moriya, Setsuko;Kiso, Makoto
我们报道了选择性人溶酶体唾液酸酶(NEU1)抑制剂的设计和合成。合成了一系列酰胺连接的C9修饰的DANA(2-脱氧-2，3-脱氢-N-乙酰神经氨酸)类似物，并测定了它们对四种人唾液酸酶(NEU1-NEU4)的抑制活性。用基于结构的方法研究了具有实验观察活性的化合物的选择性基础。本研究的结果为进一步设计具有治疗价值的异构型选择性人唾液酸酶抑制剂提供了定性的信息。(C)2007爱思唯尔有限公司。保留所有权利。
We here report the design and synthesis of selective human lysosomal sialidase (NEU1) inhibitors. A series of amide-linked C9 modified DANA (2-deoxy-2,3-dehydro-N-acetylneuraminic acid) analogues were synthesized and their inhibitory activities against all four human sialidases (NEU1-NEU4) were determined. Structure-based approach was used to investigate the basis of selectivity of the compounds with experimentally observed activity. Results from the present study are found to be informative in a qualitative manner for the further design of isoform selective human sialidase inhibitors for therapeutic value. (c) 2007 Elsevier Ltd. All rights reserved.