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

Authors :
Garrett Berlond Minne
Michel Surkyn
Harrie J.M. Gijsen
Francois Paul Bischoff
Nigel Austin
Marc Mercken
Didier Berthelot
Chiara Zavattaro
Ishtiyaque Ahmad
Gregor James Macdonald
Adriana Ingrid Velter
Michel Anna Jozef De Cleyn
Deborah Dhuyvetter
Sven Franciscus Anna Van Brandt
Serge Maria Aloysius Pieters
Yves Emiel Maria Van Roosbroeck
Swapan Kumar Samanta
Herman Borghys
Source :
Bioorganicmedicinal chemistry letters. 29(14)
Publication Year :
2019

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 The classical imidazole heterocycle has been replaced by a cyano group attached to an indole nucleus.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.

Details

ISSN :
14643405
Volume :
29
Issue :
14
Database :
OpenAIRE
Journal :
Bioorganicmedicinal chemistry letters
Accession number :
edsair.doi.dedup.....8d9f458af2fb6e368fbdd2185f1f9926