SYNTHESIS AND ANTICONVULSANT SCREENING OF TWO ISOMERS OF 4-[(DICHLOROPHENYL) AMINO]-4-OXO BUTENOIC ACID

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SYNTHESIS AND ANTICONVULSANT SCREENING OF TWO ISOMERS OF 4-[(DICHLOROPHENYL) AMINO] -4-OXO BUTENOIC ACID

Abstract:

Epilepsy is a public health issue worldwide. Pharmacotherapy, the widely used treatment strategy is bedeviled by several challenges such as toxicity, untoward effects and lack of selectivity. In view of this, most epileptologists agree on the need for more selective and less toxic antiepileptic drugs. 4-[(2, 4-dichlorophenyl)amino] -4-oxo butenoic acid and 4-[(3,4-dichlorophenyl)amino] -4-oxo butenoic acid were synthesized using Micheal’s addition reaction. The structures of these compounds were elucidated using spectroscopic techniques, particularly 1D and 2D NMR. The acute toxicity study was carried out using Lorke’s method and the anticonvulsant activity was studied using MES and scPTZ induced seizure tests. The median lethal dose for 4-[(2, 4-dichlorophenyl)amino] -4-oxo butenoic acid and 4-[(3,4-dichlorophenyl)amino] -4-oxo butenoic acid was found to be 288.53mg/kg and 565.69mg/kg respectively. The compounds were found to increase the mean time of recovery from seizures in MES test compared to control and there was significant decrease in the mean onset of seizures in scPTZ test compared to control. The compounds however offered no protection against seizures and are however recommended for further pharmacological screening and optimization

SYNTHESIS AND ANTICONVULSANT SCREENING OF TWO ISOMERS OF 4-[(DICHLOROPHENYL) AMINO] -4-OXO BUTENOIC ACID

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