Bulletin of the Korean Chemical Society · 2011 · 26 citations · 2 references
PharmacyMedicinal ChemistryPharmacologyNeuropharmacologyNeurotoxicologyStructure-activity RelationshipsDrug-induced NeurotoxicityHeterocyclic ChemistryStructure-activity Relationship AnalysisAnticonvulsant ActionAnticonvulsant DrugsBenzoic Acid DerivativesMass Spectral Data AnalysisNeurotoxic ActionThiadiazole ChemistryThiazole ChemistryThiazole Synthesis
A series of thiadiazole derivatives were synthesized with differently substituted benzoic acids which were cyclized to give differently substituted thiazolidin-4-one. Elemental analysis, IR, <TEX>$^1H$</TEX> NMR, <TEX>$^{13}C$</TEX> NMR and mass spectral data confirmed the structure of the synthesized compounds. The derivatives of these moieties were evaluated for anticonvulsant activity by MES model and neurotoxicity by rotarod method. The synthesized compounds showed good potential for anticonvulsant activity besides this, the compounds also showed neurotoxic effect. It was observed that compounds with <TEX>$OCH_3$</TEX> at 3, 4 position of phenyl ring [5(a-l)] showed less protection against convulsions as compared to compounds having unsubstituted phenyl ring [4(a-l)].
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Antiepileptic Drug Development: II. Anticonvulsant Drug Screening
Ronald L Krall, J. K. Penry, B. G. White et al. · Epilepsia · 1978 · 823 citations