2. Academic Validation
  3. Design and synthesis of a novel series of cyanoindole derivatives as potent γ-secretase modulators

Design and synthesis of a novel series of cyanoindole derivatives as potent γ-secretase modulators

  • Bioorg Med Chem Lett. 2019 Jul 15;29(14):1737-1745. doi: 10.1016/j.bmcl.2019.05.023.
François P Bischoff 1,  Adriana Ingrid Velter 2,  Garrett Minne 2,  Serge Pieters 2,  Didier Berthelot 2,  Michel De Cleyn 2,  Harrie J M Gijsen 2,  Gregor Macdonald 2,  Michel Surkyn 2,  Sven Van Brandt 2,  Yves Van Roosbroeck 2,  Chiara Zavattaro 2,  Marc Mercken 2,  Nigel Austin 2,  Deborah Dhuyvetter 2,  Herman Borghys 2,  Ishtiyaque Ahmad 3,  Swapan Kumar Samanta 3
Affiliations

Affiliations

  • 1 Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium. Electronic address: [email protected].
  • 2 Janssen Research & Development, Turnhoutseweg 30, 2340 Beerse, Belgium.
  • 3 Jubilant Biosys Ltd, Bangalore, Karnataka, India.
PMID: 31122869 DOI: 10.1016/j.bmcl.2019.05.023
Abstract

The discovery, design and synthesis of a new series of GSMs is described. The classical imidazole heterocycle has been replaced by a cyano group attached to an indole nucleus. The exploration of this series has led to compound 26-S which combined high in vitro and in vivo potency with an acceptable drug-like profile.

Keywords

Alzheimer’s disease; GSMs; γ-Secretase; γ-Secretase modulators.

Figures
Products