Initial Optimization of a New Series of γ-Secretase Modulators Derived from a Triterpene Glycoside.

ABSTRACT: The discovery of a new series of γ-secretase modulators is disclosed. Starting from a triterpene glycoside γ-secretase modulator that gave a very low brain-to-plasma ratio, initial SAR and optimization involved replacement of a pendant sugar with a series of morpholines. This modification led to two compounds with significantly improved central nervous system (CNS) exposure.

SUBMITTER: Fuller NO 

PROVIDER: S-EPMC4025870 | biostudies-literature | 2012 Nov

REPOSITORIES: biostudies-literature