Substituted indole-2-carboxylates as potent antagonists of the glycine binding site associated with the NMDA receptor.
A novel series of indole-2-carboxylate analogues of GV150526 (1) in which the propenoic double bond was substituted with different "probes" or replaced by a isosteric cyclopropyl moiety were synthesized and evaluated for their affinity profile in order to obtain further information on the pharmacophoric model of the glycine binding site associated to the NMDA receptor.
Micheli
F
F
Glaxo Wellcome S.p.A., Medicines Research Centre, Verona, Italy.
Di Fabio
R
R
Baraldi
D
D
Conti
N
N
Cugola
A
A
Gastaldi
P
P
Giacobbe
S
S
Marchioro
C
C
Mugnaini
M
M
Rossi
L
L
Pecunioso
A
A
Pentassuglia
G
G
D000818:Animals; D001665:Binding Sites / Q000187:drug effects*; D005998:Glycine / Q000037:antagonists & inhibitors* / Q000378:metabolism; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D051379:Mice; D016194:Receptors, N-Methyl-D-Aspartate / Q000378:metabolism*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D007211:Indoles; D016194:Receptors, N-Methyl-D-Aspartate; D005998:Glycine