Synthesis of GABA-valproic acid derivatives and evaluation of their anticonvulsant and antioxidant activity.
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 (RM) and calculated (sigma f and log PSK) lipophilicity for this series of compounds.
Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, Greece.
G V
GV
Rekatas
E
E
Tani
V J
VJ
Demopoulos
P N
PN
Kourounakis
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology; D000975:Antioxidants / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D051381:Rats; D011916:Rats, Inbred F344; D014635:Valproic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D005680:gamma-Aminobutyric Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis
D000927:Anticonvulsants; D000975:Antioxidants; D005680:gamma-Aminobutyric Acid; D014635:Valproic Acid