Short communication, Note

https://doi.org/10.2478/v10007-008-0025-0

Synthesis, anticonvulsant and toxicity evaluation of 2-(1H-indol-3-ylacetyl)-N-(substituted phenyl)hydrazinecarbothioamides and their related heterocyclic derivatives

NADEEM SIDDIQUI ; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), New Delhi-110062, India
M. SHAMSHER ALAM ; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), New Delhi-110062, India
WAQUAR AHSAN ; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), New Delhi-110062, India

Abstract

A series of new 5-(1H-indol-3-yl)methyl-4-(substituted aryl)-2,4-dihydro-3H-1,2,4-triazole-3-thiones (4a-g), 5-(1H-indol-3-yl)methyl-N-(substituted aryl)-1,3,4-oxadiazol-2-amines (5a-g) and 5-(1H-indol-3-yl)methyl-N-(substituted aryl)-1,3,4-thiadiazol-2-amines (6a-g) were prepared by treating 2-(1H-indol-3-yl)acetyl-N-(substituted phenyl)hydrazine 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.

Keywords

indoles; triazoles; thiadiazoles; oxadiazoles; anticonvulsants; neurotoxicity

Hrčak ID:

26799

URI

https://hrcak.srce.hr/26799

Publication date:

1.12.2008.

Article data in other languages: croatian

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