Design and synthesis of a novel series of cyanoindole derivatives as potent γ-secretase modulators. Issue 14 (15th July 2019) - Bischoff, François P.
Graphical abstract: 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 The classical imidazole heterocycle has been replaced by a cyano group attached to an indole nucleus.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.