159054-22-5Relevant academic research and scientific papers
Substituted indole-2-carboxylates as potent antagonists of the glycine binding site associated with the NMDA receptor
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
, p. 271 - 278 (2007/10/03)
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.
New synthesis of substituted 2-carboxyindole derivatives: Versatile introduction of a carbamoylethynyl moiety at the C-3 position
Hewkin, Cheryl T.,Di Fabio, Romano,Conti, Nadia,Cugola, Alfredo,Gastaldi, Paola,Micheli, Fabrizio,Quaglia, Anna M.
, p. 55 - 58 (2007/10/03)
A novel series of 3-carbamoylethynyl-2-carboxyindoles, antagonists acting at the strychnine-insensitive glycine binding site associated with the NMDA receptor, has been synthesised. This new versatile approach involves the introduction of a 2-chloroethenyl moiety in position C-3 with subsequent derivatisation of the terminal carboxyl group, followed by an unusual elimination of HCl to afford the ethynyl functionality. This novel series of glycine antagonists was evaluated in terms of in vitro affinity at the glycine binding site and the most potent compound was tested in vivo in the NMDA-induced convulsions model in mice.
