2. Academic Validation
  3. Discovery of fused 5,6-bicyclic heterocycles as γ-secretase modulators

Discovery of fused 5,6-bicyclic heterocycles as γ-secretase modulators

  • Bioorg Med Chem Lett. 2011 Jan 15;21(2):664-9. doi: 10.1016/j.bmcl.2010.12.012.
Jun Qin 1,  Pawan Dhondi,  Xianhai Huang,  Mihirbaran Mandal,  Zhiqiang Zhao,  Dmitri Pissarnitski,  Wei Zhou,  Robert Aslanian,  Zhaoning Zhu,  William Greenlee,  John Clader,  Lili Zhang,  Mary Cohen-Williams,  Nicholas Jones,  Lynn Hyde,  Anandan Palani
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. jun.qin@merck.com
PMID: 21195610 DOI: 10.1016/j.bmcl.2010.12.012
Abstract

We herein report the discovery of four series of fused 5,6-bicyclic heterocycles as γ-secretase modulators. Synthesis and SAR of these series are discussed. These compounds represent a new class of γ-secretase modulators that demonstrate moderate to good in vitro potency in inhibiting Aβ(42) production.

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