5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors.
5-Aryl-4-carboxamide-1,3-oxazoles are a novel, potent and selective series of GSK-3 inhibitors. The optimization of the series to yield compounds with cell activity and brain permeability is described.
Department of Medicinal Chemistry, Neuroscience Centre of Excellence of Drug Discovery, GlaxoSmithKline, Via A Fleming 4, 37135 Verona, Italy.
Gabriella
G
Gentile
Giancarlo
G
Merlo
Alfonso
A
Pozzan
Giovanni
G
Bernasconi
Benjamin
B
Bax
Paul
P
Bamborough
Angela
A
Bridges
Paul
P
Carter
Margarete
M
Neu
Gang
G
Yao
Caroline
C
Brough
Geoffrey
G
Cutler
Aaron
A
Coffin
Svetlana
S
Belyanskaya
D000818:Animals; D001714:Bipolar Disorder / Q000188:drug therapy; D001921:Brain / Q000378:metabolism; D038362:Glycogen Synthase Kinase 3 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D008958:Models, Molecular; D010080:Oxazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
D010080:Oxazoles; D047428:Protein Kinase Inhibitors; D038362:Glycogen Synthase Kinase 3