126751-17-5Relevant academic research and scientific papers
Synthesis, anticonvulsant and toxicity screening of thiazolyl-thiadiazole derivatives
Siddiqui, Nadeem,Ahsan, Waquar
, p. 261 - 268 (2012/02/13)
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.
Triazole incorporated thiazoles as a new class of anticonvulsants: Design, synthesis and in vivo screening
Siddiqui, Nadeem,Ahsan, Waquar
experimental part, p. 1536 - 1543 (2010/06/16)
Various 3-[4-(substituted phenyl)-1,3-thiazol-2-ylamino]-4-(substituted phenyl)-4,5-dihydro-1H-1,2,4-triazole-5-thiones (7a-t) were designed keeping in view the structural requirements suggested in the pharmacophore model for anticonvulsant activity. Thiazole and triazole 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). Two compounds 7d and 7f showed significant anticonvulsant activity in both the screens with ED50 values 23.9?mg/kg and 13.4?mg/kg respectively in MES screen and 178.6?mg/kg and 81.6?mg/kg respectively in scPTZ test. They displayed a wide margin of safety with Protective index (PI), median hypnotic dose (HD50) and median lethal dose (LD50) much higher than the standard drugs.
