Abstract
Semicarbazones are synthesized by the condensation of semicarbazide and aldehyde/ketone. The literature survey revealed that semicarbazones had been emerged as compounds with diverse biological activities including anticonvulsant, antitubercular, anticancer, and antimicrobial activities. The anticonvulsant activity of semicarbazones is mainly attributed due to the presence of an aryl binding site with aryl/alkyl hydrophobic group, a hydrogen bonding domain and an electron donor group and they are suggested to act by inhibiting sodium ion (Na+) channel. Dimmock et al., reported an extensive series of semicarbazones and reported 4-(4-fluorophenoxy) benzaldehyde semicarbazone (C0102862, V102862) as lead molecule. In MES (oral) screening C0102862 showed protective index (PI > 315) more than carbamazepine (PI 101), phenytoin (PI > 21.6) and valproate (PI > 2.17). This review briefly describes the information available about semicarbazone analogs and their anticonvulsant activity.
Keywords: Anticonvulsant Agents, Binding site theory, Na+ channel blocker, Pharmacophore model, Review, Semicarbazones.
Central Nervous System Agents in Medicinal Chemistry
Title:Semicarbazone Analogs as Anticonvulsant Agents: A Review
Volume: 13 Issue: 2
Author(s): Mohamed Jawed Ahsan
Affiliation:
Keywords: Anticonvulsant Agents, Binding site theory, Na+ channel blocker, Pharmacophore model, Review, Semicarbazones.
Abstract: Semicarbazones are synthesized by the condensation of semicarbazide and aldehyde/ketone. The literature survey revealed that semicarbazones had been emerged as compounds with diverse biological activities including anticonvulsant, antitubercular, anticancer, and antimicrobial activities. The anticonvulsant activity of semicarbazones is mainly attributed due to the presence of an aryl binding site with aryl/alkyl hydrophobic group, a hydrogen bonding domain and an electron donor group and they are suggested to act by inhibiting sodium ion (Na+) channel. Dimmock et al., reported an extensive series of semicarbazones and reported 4-(4-fluorophenoxy) benzaldehyde semicarbazone (C0102862, V102862) as lead molecule. In MES (oral) screening C0102862 showed protective index (PI > 315) more than carbamazepine (PI 101), phenytoin (PI > 21.6) and valproate (PI > 2.17). This review briefly describes the information available about semicarbazone analogs and their anticonvulsant activity.
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Ahsan Jawed Mohamed, Semicarbazone Analogs as Anticonvulsant Agents: A Review, Central Nervous System Agents in Medicinal Chemistry 2013; 13 (2) . https://dx.doi.org/10.2174/18715249113136660016
DOI https://dx.doi.org/10.2174/18715249113136660016 |
Print ISSN 1871-5249 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6166 |
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