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Substituted Indole‐2‐carboxylates as Potent Antagonists of the Glycine Binding Site Associated with the NMDA Receptor
Author(s) -
Micheli Fabrizio,
Di Fabio Romano,
Baraldi Davide,
Conti Nadia,
Cugola Alfredo,
Gastaldi Paola,
Giacobbe Simone,
Marchioro Carla,
Mugnaini Manolo,
Rossi Luciana,
Pecunioso Angelo,
Pentassuglia Giorgio
Publication year - 1999
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/(sici)1521-4184(19998)332:8<271::aid-ardp271>3.0.co;2-x
Subject(s) - indole test , moiety , chemistry , glycine , stereochemistry , nmda receptor , glycine receptor , carboxylate , binding site , receptor , combinatorial chemistry , biochemistry , amino acid
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.