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Quantitative Measurement of γ-Secretase-mediated Amyloid Precursor Protein and Notch Cleavage in Cell-based Luciferase Reporter Assay Platforms
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Published on: January 25, 2018

Triazoles as γ-secretase modulators.

Christian Fischer1, Susan L Zultanski, Hua Zhou

  • 1Merck Research Laboratories Boston, 33 Avenue Louis Pasteur, Boston, MA 02115, USA. christian_fischer@merck.com

Bioorganic & Medicinal Chemistry Letters
|May 28, 2011
PubMed
Summary
This summary is machine-generated.

Novel aryl triazoles effectively modulate gamma secretase activity. These compounds show excellent pharmacokinetics and reduce central amyloid-beta 42 levels in rats, offering potential for Alzheimer's disease therapeutics.

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Area of Science:

  • Medicinal Chemistry
  • Neuroscience
  • Drug Discovery

Background:

  • Gamma secretase modulators (GSMs) are investigated for Alzheimer's disease treatment.
  • Non-acidic GSMs often utilize olefin moieties.
  • Exploring alternative heterocyclic scaffolds is crucial for novel drug development.

Purpose of the Study:

  • To synthesize and evaluate novel aryl triazoles as gamma secretase modulators (GSMs).
  • To identify five-membered heterocycles as potential replacements for olefins in non-acidic GSMs.
  • To assess the in vivo efficacy of identified compounds in reducing amyloid-beta 42.

Main Methods:

  • Structure-activity relationship (SAR) studies were conducted on aryl triazole derivatives.
  • Synthesis of a range of five-membered heterocycles was performed.
  • In vivo evaluation involved assessing central amyloid-beta 42 lowering in Sprague-Dawley rats.

Main Results:

  • 1,2,3-C-aryl-triazoles were identified as effective replacements for olefins.
  • The synthesized aryl triazoles demonstrated good modulation of gamma secretase activity.
  • Compounds exhibited excellent pharmacokinetic profiles and significant central lowering of amyloid-beta 42 in vivo.

Conclusions:

  • Aryl triazoles represent a promising class of novel gamma secretase modulators.
  • These compounds offer a viable alternative to olefin-based GSMs.
  • The findings support the potential of aryl triazoles for Alzheimer's disease therapeutic strategies.