4-Aminoquinolines as a novel class of NR1/2B subtype selective NMDA receptor antagonists.
Screening of the Roche compound library led to the identification of 4-aminoquinoline 4 as structurally novel NR1/2B subtype selective NMDA receptor antagonist. The SAR which was developed in this series resulted in the discovery of highly potent and in vivo active blockers.
Pharma Division, Discovery Chemistry, F. Hoffmann-La Roche Ltd., CH-4070, Basel, Switzerland. emmanuel.pinard@roche.com
Emmanuel
E
Pinard
Alexander
A
Alanine
Anne
A
Bourson
Bernd
B
Büttelmann
Marie
M
Heitz
Vincent
V
Mutela Ramanjit Gill
Gerhard
G
Trube
René
R
Wyler
D000634:Aminoquinolines / Q000737:chemistry / Q000494:pharmacology*; D018691:Excitatory Amino Acid Antagonists / Q000737:chemistry / Q000494:pharmacology*; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D000634:Aminoquinolines; D018691:Excitatory Amino Acid Antagonists; D016194:Receptors, N-Methyl-D-Aspartate