120425-64-1Relevant articles and documents
Synthesis of N-acyl-2-pyrrolidinones from the corresponding N-acyl-GABA derivatives
Rekatas, George V.,Demopoulos, Vassilis J.,Kourounakis, Panos N.
, p. 989 - 990 (1996)
In this work, the synthesis of 1-(pyridine-3-carbonyl)pyrrolidin-2-one (1a) and 1-(2-propyl-1-pentanoyl)pyrrolidin-2-one (1b) by cyclization of the corresponding GABA derivatives, is reported. Two different methods are developed. For the synthesis of 1a, the parent molecule 4-[(pyridine-3-carbonyl)-amino]butanoic acid (2a) is treated first with thionyl chloride and then with triethylamine. The second derivative, 1b, is produced by an intramolecular dehydration of 4-(2-propylpentanoylamino)butanoic acid (2b) using an acid catalyst.
Synthesis of GABA-valproic acid derivatives and evaluation of their anticonvulsant and antioxidant activity
Rekatas, George V.,Tani, Ekaterini,Demopoulos, Vassilis J.,Kourounakis, Panos N.
, p. 393 - 398 (2007/10/03)
The synthesis and the anticonvulsant activity of a number of GABA and valproic acid derivatives are reported. The lipophilicity of these compunds 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 synthetized 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 (Σf and log P(SK)) lipophilicity for this series of compounds.
