1.
Synthesis and GABA uptake inhibitory properties of 6-aryl iminoxymethyl substituted nipecotic acids.
Eur J Med Chem
; 39(10): 889-95, 2004 Oct.
Artigo
em Inglês
| MEDLINE
| ID: mdl-15464623
RESUMO
Nipecotic acid derivatives bearing an aryl iminoxymethyl side chain at the position 6 were synthesised and tested for their GABA uptake inhibitory properties. Contrarily to the N-substituted derivatives 2, 3 the introduction of the oxime function in the side chain of analogues of the active nipecotic derivative 4 does neither increase, nor maintain the activity.
Assuntos
Ácidos Nipecóticos/síntese química , Ácidos Nipecóticos/metabolismo , Ácido gama-Aminobutírico/metabolismo , Animais , Corpo Estriado/metabolismo , GABAérgicos/síntese química , GABAérgicos/metabolismo , Ratos
2.
Eur J Med Chem
; 39(7): 633-8, 2004 Jul.
Artigo
em Inglês
| MEDLINE
| ID: mdl-15236844
RESUMO
6-aralkylether- and 6-arylenol-ether-substituted nipecotic acids were synthesized. These analogues are poor GABA uptake inhibitors. The electronegative region concept developed in the N-substituted nipecotic acid series cannot be transferred on the side chain of this series of 6-substituted analogues.