Abstract
A series of novel (±) 3-menthone semicarbazides (1-7) and thiosemicarbazides (8-14) were 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 N1 – (4-fluorophenyl) – N4- (menth-3- one) semicarbazide (4) emerged as the most active compound with MES ED50 of 44.15mg/kg and scPTZ ED50 of 38.68mg/kg at 0.25h duration. These compounds were found to elevate γ-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.
Keywords: (±) 3-menthone, semicarbazides, thiosemicarbazides, anticonvulsant, Maximal Electroshock Seizure (MES), subcutaneous pentylene tetrazole (scPTZ), Antiepileptic drug development (AED)
Medicinal Chemistry
Title: Menthone Semicarbazides and Thiosemicarbazides as Anticonvulsant Agents
Volume: 6 Issue: 1
Author(s): Jainendra Jain, Y. Kumar, James Stables and Reema Sinha
Affiliation:
Keywords: (±) 3-menthone, semicarbazides, thiosemicarbazides, anticonvulsant, Maximal Electroshock Seizure (MES), subcutaneous pentylene tetrazole (scPTZ), Antiepileptic drug development (AED)
Abstract: A series of novel (±) 3-menthone semicarbazides (1-7) and thiosemicarbazides (8-14) were 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 N1 – (4-fluorophenyl) – N4- (menth-3- one) semicarbazide (4) emerged as the most active compound with MES ED50 of 44.15mg/kg and scPTZ ED50 of 38.68mg/kg at 0.25h duration. These compounds were found to elevate γ-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.
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Cite this article as:
Jain Jainendra, Kumar Y., Stables James and Sinha Reema, Menthone Semicarbazides and Thiosemicarbazides as Anticonvulsant Agents, Medicinal Chemistry 2010; 6 (1) . https://dx.doi.org/10.2174/157340610791208727
DOI https://dx.doi.org/10.2174/157340610791208727 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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