2. Academic Validation
  3. Iminoheterocycles as gamma-secretase modulators

Iminoheterocycles as gamma-secretase modulators

  • Bioorg Med Chem Lett. 2010 Sep 15;20(18):5380-4. doi: 10.1016/j.bmcl.2010.07.121.
John P Caldwell 1,  Chad E Bennett,  Troy M McCracken,  Robert D Mazzola,  Thomas Bara,  Alexei Buevich,  Duane A Burnett,  Inhou Chu,  Mary Cohen-Williams,  Hubert Josein,  Lynn Hyde,  Julie Lee,  Brian McKittrick,  Lixin Song,  Giuseppe Terracina,  Johannes Voigt,  Lili Zhang,  Zhaoning Zhu
Affiliations

Affiliation

  • 1 Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States. john.caldwell@merck.com
PMID: 20724152 DOI: 10.1016/j.bmcl.2010.07.121
Abstract

The synthesis of a novel series of iminoheterocycles and their structure-activity relationship (SAR) as modulators of gamma-secretase activity will be detailed. Encouraging SAR generated from a monocyclic core led to a structurally unique bicyclic core. Selected compounds exhibit good potency as gamma-secretase modulators, excellent rat pharmacokinetics, and lowering of Abeta42 levels in various in vivo models.

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