Synthesis, anticonvulsant and toxicity screening of thiazolyl-thiadiazole derivatives

Various thiazole-substituted thiadiazole derivatives (7a-t) were designed and synthesized using substituted acetophenones and substituted anilines as starting materials. Thiazole and thiadiazole moieties being anticonvulsants were clubbed together to get the titled compounds and their in vivo antico...

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Veröffentlicht in:Medicinal chemistry research 2011-03, Vol.20 (2), p.261-268
Hauptverfasser: Siddiqui, Nadeem, Ahsan, Waquar
Format: Artikel
Sprache:eng
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Zusammenfassung:Various thiazole-substituted thiadiazole derivatives (7a-t) were designed and synthesized using substituted acetophenones and substituted anilines as starting materials. Thiazole and thiadiazole moieties being anticonvulsants were clubbed together to get the titled compounds and their in vivo anticonvulsant screening were performed by two most adopted seizure models, maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ). Three compounds 7i, 7l and 7n were found to be potent in both the screens with comparable ED₅₀ and better TD₅₀ values than some standard drugs. These compounds were also found to exert lesser toxic effects on liver.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-010-9313-6