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.
Pinard
Emmanuel
E
Pharma Division, Discovery Chemistry, F. Hoffmann-La Roche Ltd., CH-4070, Basel, Switzerland. emmanuel.pinard@roche.com
Alanine
Alexander
A
Bourson
Anne
A
Büttelmann
Bernd
B
Heitz
Marie
M
Mutela Ramanjit Gill
Vincent
V
Trube
Gerhard
G
Wyler
René
R
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