Molecules · 2014 · 49 citations · 23 references
MedicineMedicinal ChemistryPharmacologyMolecular PharmacologyNeuropharmacologyStructure-activity RelationshipsGabaergic NeurochemistryGabaergic PharmacologyGabaergic SignalingAnticonvulsant ActionAnticonvulsant DrugsAnticonvulsant PharmacologyGabaergic Role In EpilepsySeizures
The anticonvulsant activity of several 1,2,4-triazole-3-thione derivatives on mouse maximal electroshock-induced seizures was tested in this study. Characteristic features of all active compounds were rapid onset of action and long lasting effect. Structure-activity observations showed that the probability of obtaining compounds exerting anticonvulsant activity was much higher when at least one of the phenyl rings attached to 1,2,4-triazole nucleus had a substituent at the para position. The obtained results, moreover, permit us to conclude that despite the structural similarity of loreclezole (second-generation anticonvulsant drug) and the titled compounds, their anticonvulsant activity is achieved via completely different molecular mechanisms.
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A simplified method of evaluating dose-effect experiments.
Frank Wilcoxon · PubMed · 1949 · 2K citations
Rate-Limited Steps of Human Oral Absorption and QSAR Studies
Yuan H. Zhao, Michael H. Abraham, Joelle Le et al. · Pharmaceutical Research · 2002 · 707 citations
Correlation of Drug Absorption with Molecular Surface Properties
Katrin Palm, Krishna Luthman, Anna-Lena Unge et al. · Journal of Pharmaceutical Sciences · 1996 · 415 citations