Synthesis, anticonvulsant and toxicity evaluation of 2-1H-indol-3-ylacetyl-N-substituted phenylhydrazinecarbothioamides and their related heterocyclic derivativesReport as inadecuate




Synthesis, anticonvulsant and toxicity evaluation of 2-1H-indol-3-ylacetyl-N-substituted phenylhydrazinecarbothioamides and their related heterocyclic derivatives - Download this document for free, or read online. Document in PDF available to download.

Acta Pharmaceutica, Vol.58 No.4 December 2008. -

A series of new 5-1H-indol-3-ylmethyl-4-substituted aryl-2,4-dihydro-3H-1,2,4-triazole-3-thiones 4a-g, 5-1H-indol-3-ylmethyl-N-substituted aryl-1,3,4-oxadiazol-2-amines 5a-g and 5-1H-indol-3-ylmethyl-N-substituted aryl-1,3,4-thiadiazol-2-amines 6a-g were prepared by treating 2-1H-indol-3-ylacetyl-N-substituted phenylhydrazine carbothioamides 3a-g with suitable reagents. All the newly synthesized compounds were screened for their anticonvulsant activity in the MES model and were compared with the standard drugs phenytoin sodium and carbamazepine. Out of the twenty-one compounds studied, 4b, 4e, 4f, 5b, 5d, 5g, 6b, 6d and 6e showed comparable MES activity to phenytoin and carbamazepine after 0.5 h. Compound 5b showed to be more potent than carbamazepine after 4 h. Compounds 4a, 4c, 4d, 5a, 5c, 5e, 5f, 6f and 6g showed lower neurotoxicity than phenytoin.

indoles; triazoles; thiadiazoles; oxadiazoles; anticonvulsants; neurotoxicity



Author: NADEEM SIDDIQUI - ; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard Hamdard University, New Delhi-1100

Source: http://hrcak.srce.hr/



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