Systematic variation of membrane anchor, spacer and pharmacophore building blocks leads to an optimisation of the inhibitory effect of tripartite structures towards BACE1-induced cleavage of the amyloid precursor protein (APP).
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Optimisation of BACE1 inhibition of tripartite structures by modification of membrane anchors, spacers and pharmacophores – development of potential agents for the treatment of Alzheimer's disease
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a
Department Chemie, Technische Universität Dresden, Bergstrasse 66, 01069 Dresden, Germany
E-mail: hans-joachim.knoelker@tu-dresden.de
E-mail: hans-joachim.knoelker@tu-dresden.de
b
LVR Klinikum Essen, Klinik für Psychiatrie und Psychotherapie, Universität Duisburg-Essen, Virchowstrasse 171, 45147 Essen, Germany
E-mail: hans.klafki@uni-due.de
E-mail: hans.klafki@uni-due.de
Org. Biomol. Chem., 2012,10, 8216-8235
DOI: 10.1039/C2OB26103K
Received 07 Jun 2012, Accepted 02 Aug 2012
First published online 03 Aug 2012
Organic & Biomolecular Chemistry
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