Triazolopyrimidinones as γ-secretase modulators: structure–activity relationship, modulator profile, and in vivo profiling†‡,10.1039/C2MD20312J

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Lactoyl-CoA 全氟丁基戊烷白叶藤碱全氟己基辛烷新白叶藤碱壳寡糖特色专题-生物多肽

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

Ulrika Yngve,Kim Paulsen,Istvan Macsari,Marie Sundström,Ellen Santangelo,Christian Linde,Krisztian Bogar,Fredrik Lake,Yevgeni Besidski,Jonas Malmborg,Paulina Appelkvist,Ann-Cathrine Radesäter,Fredrik Olsson,Daniel Bergström,Rebecka Klintenberg

MedChemComm Pub Date : 01/10/2013 00:00:00 , DOI:10.1039/C2MD20312J

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.