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Issue 2, 2013
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Triazolopyrimidinones as γ-secretase modulators: structure–activity relationship, modulator profile, and in vivo profiling

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Abstract

The structure–activity relationship for a series of potent γ-secretase modulators based on the 6,7-dihydro-4H-[1,2,4]triazolo[1,5-a]pyrimidin-5-one scaffold is described. Furthermore, we report details regarding the modulator profile on Aβ processing, as well as in vivo efficacy, for the optimized compounds.

Graphical abstract: Triazolopyrimidinones as γ-secretase modulators: structure–activity relationship, modulator profile, and in vivo profiling

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Article information


Submitted
12 Oct 2012
Accepted
19 Nov 2012
First published
10 Jan 2013

Med. Chem. Commun., 2013,4, 422-431
Article type
Concise Article

Triazolopyrimidinones as γ-secretase modulators: structure–activity relationship, modulator profile, and in vivo profiling

U. Yngve, K. Paulsen, I. Macsari, M. Sundström, E. Santangelo, C. Linde, K. Bogar, F. Lake, Y. Besidski, J. Malmborg, K. Strömberg, P. Appelkvist, A. Radesäter, F. Olsson, D. Bergström, R. Klintenberg and P. I. Arvidsson, Med. Chem. Commun., 2013, 4, 422
DOI: 10.1039/C2MD20312J

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