Design and optimization of tricyclic gamma-secretase modulators

Jianliang Shi,Dmitry Zuev, Li Xu,Kimberley A Lentz,James E Grace,Jeremy H Toyn,Richard E Olson,John E Macor,Lorin A Thompson

Bioorganic & Medicinal Chemistry Letters（2016）

引用 12|浏览46

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摘要

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.

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关键词

Alzheimer’s disease,Gamma-secretase modulators,CYP3A4 inhibition

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