1.
Synthesis and GABA uptake inhibitory properties of 6-aryl iminoxymethyl substituted nipecotic acids.
Eur J Med Chem
; 39(10): 889-95, 2004 Oct.
Article
in English
| MEDLINE
| ID: mdl-15464623
ABSTRACT
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.
Subject(s)
Nipecotic Acids/chemical synthesis , Nipecotic Acids/metabolism , gamma-Aminobutyric Acid/metabolism , Animals , Corpus Striatum/metabolism , GABA Agents/chemical synthesis , GABA Agents/metabolism , Rats
2.
Eur J Med Chem
; 39(7): 633-8, 2004 Jul.
Article
in English
| MEDLINE
| ID: mdl-15236844
ABSTRACT
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.