65036-57-9Relevant articles and documents
HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF
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Page/Page column 136, (2011/12/14)
Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes
Improved method for preparing 1-amino-3,7,8-trichlorodibenzo-p-dioxin
Ledentsova,Suslova,Antonov,Pavlova,Nikonova,Borob'ev-Desyatovskii
, p. 2037 - 2039 (2007/10/03)
An improved method was proposed for preparing 1-amino-3,7,8-trichlorodibenzo-p-dioxin.
Potent Quinoxaline-Spaced Phosphono α-Amino Acids of the AP-6 Type as Competitive NMDA Antagonists: Synthesis and Biological Evaluation
Baudy, Reinhardt B.,Greenblatt, Lynne P.,Jirkovsky, Ivo L.,Conklin, Mary,Russo, Ralph J.,et al.
, p. 331 - 342 (2007/10/02)
A series of α-amino-3-(phosphonoalkyl)-2-quinoxalinepropanoic acids was synthesized and evaluated for NMDA receptor affinity using a CPP binding assay.Functional antagonism of the NMDA receptor complex was evaluated in vitro using a stimulated TCP binding assay and in vivo by empolying an NMDA-induced seizure model.Some analogues also were evaluated in the -glycine binding assay.Several compounds of the AP-6 type show potent and selective NMDA antagonistic activity both in vitro and in vivo.In particular α-amino-7-chloro-3-(phosphonomethyl)-2-quinoxalinepropanoic acid (1) d isplayed an ED50 of 1.1 mg/kg ip in the NMDA lethality model.Noteworthy is α-amino-6,7-dichloro-3-(phosphonomethyl)-2-quinoxalinepropanoic acid (3) with a unique dual activity, displaying in the NMDA receptor binding assay an IC50 of 3.4 nM and in the glycine binding assay an IC50 of 0.61 μM.