Synthesis and structure-activity relationship of a novel series of heterocyclic sulfonamide γ-secretase inhibitors
Synthesis and structure-activity relationship of a novel series of heterocyclic sulfonamide γ-secretase inhibitors
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DOI：
10.1016/j.bmc.2009.04.052
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发表时间：
2009-07-01
影响因子：
3.5
通讯作者：
Resnick, Lynn
中科院分区：
文献类型：
--
作者：
Pu, Jun;Kreft, Anthony F.;Resnick, Lynn
-分泌酶抑制剂已被证明可以减少β -淀粉样蛋白的产生，β -淀粉样蛋白是阿尔茨海默病患者大脑中发现的斑块的一种成分。报道了一系列新的杂环磺胺γ分泌酶抑制剂，可降低细胞中的β -淀粉样蛋白水平。本系列化合物中的几个例子表明，与Notch（另一种γ分泌酶底物）相比，Notch具有更高的抑制淀粉样蛋白前体蛋白加工的倾向。2009爱思唯尔有限公司版权所有。
gamma-Secretase inhibitors have been shown to reduce the production of beta-amyloid, a component of the plaques that are found in brains of patients with Alzheimer's disease. A novel series of heterocyclic sulfonamide gamma-secretase inhibitors that reduce beta-amyloid levels in cells is reported. Several examples of compounds within this series demonstrate a higher propensity to inhibit the processing of amyloid precursor protein compared to Notch, an alternative gamma-secretase substrate. (C) 2009 Elsevier Ltd. All rights reserved.