2. Academic Validation
  3. Membrane anchoring γ-secretase modulators with terpene-derived moieties

Membrane anchoring γ-secretase modulators with terpene-derived moieties

  • Bioorg Med Chem Lett. 2013 Jul 1;23(13):3852-6. doi: 10.1016/j.bmcl.2013.04.070.
Eva Christine Naumann 1,  Stefan Göring,  Isabella Ogorek,  Sascha Weggen,  Boris Schmidt
Affiliations

Affiliation

  • 1 Clemens Schöpf-Institute of Organic Chemistry and Biochemistry, Technische Universität Darmstadt, 64287 Darmstadt, Germany.
PMID: 23707256 DOI: 10.1016/j.bmcl.2013.04.070
Abstract

Modulation of γ-secretase activity is a promising therapeutic strategy for the treatment of Alzheimer's disease. Herein we report on the synthesis of carprofen- and tocopherol-derived small-molecule modulators carrying terpene moieties as lipophilic membrane anchors. Additionally, these modulators are equipped with an acidic moiety, which contributes to the desired modulatory effect on the γ-secretase with decreased formation of Aβ42 and increased Aβ38 production.

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