Initial Optimization of a New Series of γ-Secretase Modulators Derived from a Triterpene Glycoside
ACS Medicinal Chemistry Letters2012Vol. 3(11), pp. 908–913
Citations Over TimeTop 23% of 2012 papers
Nathan O. Fuller, Jed L. Hubbs, Wesley Austin, Steffen P. Creaser, Timothy D. McKee, Robyn Loureiro, Barbara Tate, Weiming Xia, Jeffrey L. Ives, Mark A. Findeis, Brian S. Bronk
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.
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