3-(2-Carbamoylvinyl)-4,5-dimethylpyrrole-2-carboxylic acids as ligands at the NMDA glycine-binding site: a study on the 2-carbamoylvinyl chain modification.
Farmaco
; 54(1-2): 101-11, 1999.
Article
em En
| MEDLINE
| ID: mdl-10321036
ABSTRACT
Twenty 4,5-dimethylpyrrole-2-carboxylic acids (5a-t) with different 2-carbamoylvinyl chains in position 3 were prepared to further investigate the relationships between structure and in vitro affinity for the strychnine-insensitive glycine-binding site. None of these compounds was superior to (E)-3-(N-phenyl-2-carbamoylvinyl)-4,5-dimethylpyrrole-2-carb oxylic acid III (pKi = 6.70), which was taken as a reference standard, but overall the results obtained indicate that the N-phenyl-2-carbamoylvinyl substituent of III may be replaced with the N-(1-adamantyl)-2-carbamoylvinyl group as in 5h (pKi = 6.20) without considerable loss of affinity. This finding adds to previous knowledge.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Pirróis
/
Ácidos Carboxílicos
/
Receptores de N-Metil-D-Aspartato
/
Glicinérgicos
Limite:
Animals
Idioma:
En
Revista:
Farmaco
Assunto da revista:
FARMACOLOGIA
/
QUIMICA
Ano de publicação:
1999
Tipo de documento:
Article
País de afiliação:
Itália