1-Benzyloxy-4,5-dihydro-1H-imidazol-2-yl-amines, a novel class of NR1/2B subtype selective NMDA receptor antagonists.
Screening of the Roche compound depository led to the identification of (1-benzyloxy-4,5-dihydro-1H-imidazol-2-yl)-butyl amine 4, a structurally novel NR1/2B subtype selective NMDA receptor antagonist. The structure-activity relationships developed in this series resulted in the discovery of a novel class of potent and selective NMDA receptor blockers displaying activity in vivo.
Alanine
Alexander
A
Pharma Division, Discovery Chemistry, F. Hoffmann-La Roche Ltd., CH-4070 Basel, Switzerland. alexander.alanine@roche.com
Bourson
Anne
A
Büttelmann
Bernd
B
Gill
Ramanjit
R
Heitz
Marie Paule
MP
Mutel
Vincent
V
Pinard
Emmanuel
E
Trube
Gerhard
G
Wyler
René
R
D000818:Animals; D002478:Cells, Cultured; D018691:Excitatory Amino Acid Antagonists / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D007093:Imidazoles / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D007274:Injections, Intraperitoneal; D051379:Mice; D008811:Mice, Inbred DBA; D024642:Potassium Channels, Voltage-Gated / Q000037:antagonists & inhibitors; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors* / Q000502:physiology; D012640:Seizures / Q000517:prevention & control
D018691:Excitatory Amino Acid Antagonists; D007093:Imidazoles; C409466:NR1 NMDA receptor; C121001:NR2B NMDA receptor; D024642:Potassium Channels, Voltage-Gated; D016194:Receptors, N-Methyl-D-Aspartate