Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 23, Issue 17, Pages 4794-4800Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.06.100
Keywords
Alzheimer's disease; gamma-Secretase modulators
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The evolution of amide 3 into conformationally restricted bicyclic triazolo-piperidine 14-S as a gamma-secretase modulator is described. This is a potential disease modifying anti-Alzheimer's drug which demonstrated high in vitro and in vivo potency against A beta 42 peptide, reduced lipophilicity and enhanced brain free fraction compared to the previous series. (C) 2013 Elsevier Ltd. All rights reserved.
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