Premium
Synthesis of GABA‐Valproic Acid Derivatives and Evaluation of Their Anticonvulsant and Antioxidant Activity
Author(s) -
Rekatas George V.,
Tani Ekaterini,
Demopoulos Vassilis J.,
Kourounakis Panos N.
Publication year - 1996
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19963290804
Subject(s) - lipophilicity , anticonvulsant , chemistry , valproic acid , lipid peroxidation , antioxidant , inhibitory postsynaptic potential , biological activity , stereochemistry , pharmacology , biochemistry , in vitro , epilepsy , medicine , neuroscience , biology
The synthesis and the anticonvulsant activity of a number of GABA and valproic acid derivatives are reported. The lipophilicity of these compounds and their inhibitory effect on lipid peroxidation were also investigated, in an effort to correlate the anticonvulsant activity with lipophilicity and inhibitory effect on lipid peroxidation. The synthesized compounds exhibited anticonvulsant effects which were stronger for the more lipophilic derivatives. One of the active anticonvulsants showed appreciable antioxidant properties. Finally, a good correlation was found between the experimentally derived ( R M ) and calculated (σ and log P SK ) lipophilicity for this series of compounds.