Abstract
A series of semicarbazones and thiosemicarbazones were designed and synthesized to meet the structural requirements essential for anticonvulsant activity. All the compounds were evaluated for anticonvulsant activity after intraperitoneal (i.p.) administration to mice by maximal electroshock (MES) and subcutaneous metrazol (ScMet) induced seizure methods and minimal motor impairment was determined by rotorod test. Semicarbazones and thiosemicarbazones of lipophillic carbonyl groups (citral and carvone) showed excellent activity while semicarbazone and thiosemicarbazone of levulinic acid were found to be inactive. Results of the present study show that lipophilic aryl ring could be replaced with non-cyclic lipophillic groups but could not be replaced with hydrophilic substituents.
Keywords: Anticonvulsant, semicarbazones, thiosemicarbazones
Central Nervous System Agents in Medicinal Chemistry
Title: Design and Evaluation of Semicarbazones and Thiosemicarbazones as Novel Anticonvulsants
Volume: 8 Issue: 1
Author(s): Navneet Aggarwal, Ruchi Aggarwal, Pradeep Mishra, J. S. Jain, S. K. Bansal and K. K. Jha
Affiliation:
Keywords: Anticonvulsant, semicarbazones, thiosemicarbazones
Abstract: A series of semicarbazones and thiosemicarbazones were designed and synthesized to meet the structural requirements essential for anticonvulsant activity. All the compounds were evaluated for anticonvulsant activity after intraperitoneal (i.p.) administration to mice by maximal electroshock (MES) and subcutaneous metrazol (ScMet) induced seizure methods and minimal motor impairment was determined by rotorod test. Semicarbazones and thiosemicarbazones of lipophillic carbonyl groups (citral and carvone) showed excellent activity while semicarbazone and thiosemicarbazone of levulinic acid were found to be inactive. Results of the present study show that lipophilic aryl ring could be replaced with non-cyclic lipophillic groups but could not be replaced with hydrophilic substituents.
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Aggarwal Navneet, Aggarwal Ruchi, Mishra Pradeep, Jain S. J., Bansal K. S. and Jha K. K., Design and Evaluation of Semicarbazones and Thiosemicarbazones as Novel Anticonvulsants, Central Nervous System Agents in Medicinal Chemistry 2008; 8 (1) . https://dx.doi.org/10.2174/187152408783790596
DOI https://dx.doi.org/10.2174/187152408783790596 |
Print ISSN 1871-5249 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6166 |
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