Design and optimization of tricyclic gamma-secretase modulators

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• 作者：Jianliang Shi ; ^{jianling.shi@bms.com" class="auth_mail" title="E-mail the corresponding author} ; Dmitry Zuev ; Li Xu ; Kimberley A. Lentz ; James E. Grace ; Jeremy H. Toyn ; Richard E. Olson ; John E. Macor ; Lorin A. Thompson
• 关键词：Alzheimer&rsquo ; s disease ; Gamma-secretase modulators ; CYP3A4 inhibition
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 March 2016
• 年：2016
• 卷：26
• 期：5
• 页码：1498-1502
• 全文大小：2009 K

文摘

Beginning with a diaminotriazine screening hit, several series of novel, tricyclic gamma-secretase modulators (GSMs) were designed. The SAR of several related series of GSMs is presented, and the in vivo profile of a lead molecule from the series is described.