Journal Article10.1002/ARDP.19963290804
Synthesis of GABA-valproic acid derivatives and evaluation of their anticonvulsant and antioxidant activity.
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TL;DR: A good correlation was found between the experimentally derived (RM) and calculated (σ and log PSK) lipophilicity for this series of compounds.
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Abstract: 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.
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New CNS-active drugs which are second-generation valproic acid: can they lead to the development of a magic bullet?
TL;DR: Three compounds in clinical trials in patients with epilepsy that can be regarded as second-generation VPA: valproyl glycinamide, 3-methylbutanamide or isovaleramide and SPD421 (DP-VPA).
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Novel-Substituted Heterocyclic GABA Analogues. Enzymatic Activity against the GABA-AT Enzyme from Pseudomonas fluorescens and In Silico Molecular Modeling.
Erika Tovar-Gudiño,Juan Alberto Guevara-Salazar,José Raúl Bahena-Herrera,José G. Trujillo-Ferrara,Zuleyma Martínez-Campos,Rodrigo Said Razo-Hernández,Ángel Santiago,Nina Pastor,Mario Fernández-Zertuche +8 more
TL;DR: Some new analogues of GABA are designed and evaluated in vitro and in silico, where the nitrogen atom at the γ-position is embedded in heterocyclic scaffolds and determined their inhibitory potential over the GABA-AT enzyme from Pseudomonas fluorescens.
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2D and 3D QSAR analysis of some valproic acid metabolites and analogues as anticonvulsant agents.
TL;DR: It was established that the two approaches—2D and 3D QSAR, prove the importance of the lipophilicity of the compounds foranticonvulsant activity and the results from both the approaches suggest that a substitution at α-position is essential for a higher activity.
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QSAR and Molecular Docking Studies of the Inhibitory Activity of Novel Heterocyclic GABA Analogues over GABA-AT.
Josué Rodríguez-Lozada,Erika Tovar-Gudiño,Juan Alberto Guevara-Salazar,Rodrigo Said Razo-Hernández,Ángel Santiago,Nina Pastor,Mario Fernández-Zertuche +6 more
TL;DR: In vivo studies with PTZ-induced seizures on male CD1 mice show that compound 9b has a neuroprotective effect at a 0.50 mmole/kg dose, which indicates that bulky ligands tend to be the better inhibitors especially those with a sulfur atom on their structure.
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