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Arch Pharm (Weinheim). 2012 Sep;345(9):703-12. doi: 10.1002/ardp.201200014. Epub 2012 Jun 14.

Synthesis of some azoles incorporating a sulfonamide moiety as anticonvulsant agents.

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  • 1Faculty of Science, Chemistry Department, Al-Azhar University (Girls), Cairo, Egypt.

Abstract

Many derivatives of heterocyclic compounds containing a sulfonamide thiazole moiety were synthesized through the reaction of 2-(cyano or chloro)-N-(4-(N-thiazol-2-ylsulfamoyl)phenyl)acetamide with isocyanate followed by halogenated compounds, arylidene, 2-hydroxy benzaldehydes, active methylene compounds, and heterocyclic amines. The anticonvulsant activity for 15 of the synthesized compounds was evaluated and 6 compounds showed protection against picrotoxin-induced convulsion. 4-(6-Amino-3,5-dicyano-4-(4-methoxyphenyl)-2-oxopyridin-1(2H)-yl)-N-(thiazol-2-yl)benzenesulfonamide (11b) exhibited significant anticonvulsive effects, abolished the tonic extensor phase and offered 100% protection.

Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

PMID:
22696252
[PubMed - indexed for MEDLINE]
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