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Bioorg Med Chem Lett
; 26(23): 5836-5841, 2016 12 01.
Article
in English
| MEDLINE
| ID: mdl-27836402
ABSTRACT
In this paper we describe our strategy to improve the aqueous solubility of SCH 900229, a potent PS1-selective γ-secretase inhibitor for the treatment of Alzheimer's disease. Incorporation of ionizable amino groups into the side chain terminal generates water soluble ß-aminosulfone analogues of SCH 900229 that maintain robust in vitro potency and in vivo efficacy.