Iminoheterocycles as γ-secretase modulators

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• 作者：John P. Caldwell ; Chad E. Bennett ; Troy M. McCracken ; Robert D. Mazzola ; Thomas Bara ; Alexei Buevich ; Duane A. Burnett ; Inhou Chu ; Mary Cohen-Williams ; Hubert Josein ; Lynn Hyde ; Julie Lee ; Brian McKit
• 关键词：Alzheimer’ ; s disease ; γ ; -Secretase modulators
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2010
• 出版时间：15 September 2010
• 年：2010
• 卷：20
• 期：18
• 页码：5380-5384
• 全文大小：570 K

文摘

The synthesis of a novel series of iminoheterocycles and their structure–activity relationship (SAR) as modulators of γ-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 γ-secretase modulators, excellent rat pharmacokinetics, and lowering of Aβ₄₂ levels in various in vivo models.