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Menthone Semicarbazides and Thiosemicarbazides as Anticonvulsant Agents
- Source :
- Medicinal Chemistry. 6:44-50
- Publication Year :
- 2010
- Publisher :
- Bentham Science Publishers Ltd., 2010.
-
Abstract
- A series of novel (+/-) 3-menthone semi carbazides (1-7) and thiosemicarbazides synthesized using an appropriate synthetic route and characterized by thin layer chromatography and spectral analysis. The anticonvulsant activity of synthesized compounds was established after intraperitoneal administration in three seizure models in mice which include maximal electroshock seizure (MES), subcutaneous pentylene tetrazole (scPTZ) induced seizure and minimal neurotoxicity test. Seven compounds exhibited protection in both models and N(1) - (4-fluorophenyl) - N(4)- (menth-3-one) semicarbazide (4) emerged as the most active compound with MES ED(50) of 44.15mg/kg and scPTZ ED(50) of 38.68mg/kg at 0.25h duration. These compounds were found to elevate gamma-amino butyric acid (GABA) levels in the midbrain region, thus indicating that (+/-) 3-menthone semicarbazides could be considered as a lead molecule in designing of a potent anticonvulsant drug.
- Subjects :
- Male
Semicarbazide
Semicarbazides
Chemistry
medicine.medical_treatment
Cell Membrane
Pharmacology
Menthone
Thin-layer chromatography
Rats
Butyric acid
Menthol
Mice
chemistry.chemical_compound
Anticonvulsant Agent
Anticonvulsant
Drug Discovery
medicine
Animals
Anticonvulsants
Tetrazole
Hydrophobic and Hydrophilic Interactions
gamma-Aminobutyric Acid
Subjects
Details
- ISSN :
- 15734064
- Volume :
- 6
- Database :
- OpenAIRE
- Journal :
- Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....ba9928f9abbc49344fd42cc0d53d2355