Development of novel N-3-bromoisoxazolin-5-yl substituted 2,3-benzodiazepines as noncompetitive AMPAR antagonists.
Bioorg Med Chem
; 25(14): 3631-3637, 2017 07 15.
Article
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| MEDLINE
| ID: mdl-28571973
ABSTRACT
In this work, we designed and synthesized novel N-3-bromoisoxazolin-5-yl substituted 2,3-benzodiazepines as noncompetitive AMPAR antagonists, with the aim that this heterocycle could establish favourable interactions with a putative binding pocket of the receptor, like the thiadiazole nucleus of GYKI 47409 does. Within this investigation, we identified some active molecules and, among these 2,3-benzodiazepines, 4c showed a much improved inhibitory potency as compared with unsubstituted 2,3-benzodiazepines.
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Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Benzodiazepinas
/
Receptores AMPA
Límite:
Humans
Idioma:
En
Año:
2017
Tipo del documento:
Article