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

Design and optimization of tricyclic gamma-secretase modulators

2016

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

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.

Keywords:

Molecule
Amyloid precursor protein secretase
Biochemistry
Gamma secretase
Chemistry
In vivo
Tricyclic
Structure–activity relationship
Stereochemistry
Aniline Compounds

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