亚氨基杂环作为γ-分泌酶调节剂。
Iminoheterocycles as gamma-secretase modulators.
机构信息
Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States.
出版信息
Bioorg Med Chem Lett. 2010 Sep 15;20(18):5380-4. doi: 10.1016/j.bmcl.2010.07.121. Epub 2010 Aug 1.
PMID:20724152
Abstract
The synthesis of a novel series of iminoheterocycles and their structure-activity relationship (SAR) as modulators of gamma-secretase activity will be detailed. Encouraging SAR generated from a monocyclic core led to a structurally unique bicyclic core. Selected compounds exhibit good potency as gamma-secretase modulators, excellent rat pharmacokinetics, and lowering of Abeta42 levels in various in vivo models.
摘要
将详细介绍一系列新型亚氨基杂环及其作为γ-分泌酶活性调节剂的结构-活性关系（SAR）。从单环核心产生的令人鼓舞的 SAR 导致了结构独特的双环核心。选定的化合物表现出作为γ-分泌酶调节剂的良好效力、优异的大鼠药代动力学特性，并在各种体内模型中降低 Abeta42 水平。
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