Synthesis of indazole substituted-1,3,4-thiadiazoles and their anticonvulsant activity

Harish, K. P. and Mohana, K. N. and Mallesha, L. (2013) Synthesis of indazole substituted-1,3,4-thiadiazoles and their anticonvulsant activity. Drug Invention Today, 5 (2). pp. 92-99. ISSN 0975-7619

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Abstract

Objectives: To synthesize a new series of indazole substituted-1,3,4-thiadiazole derivatives 7(a-l) and test the anticonvulsant activity against maximal electroshock (MES) seizure model in male Wistar rats. Methods: New compounds were synthesized by the reaction of indazole substituted-1,3,4-thiadiazoles with various sulfonyl chlorides. The purity of the compounds was confirmed on the basis of their elemental analysis. Chemical structures of all the new compounds were established by 1H NMR and mass spectral data. Anticonvulsant study was done by MES seizure model and rotorod method was employed to determine the neurotoxicity. Results: All the compounds were synthesized in good yield. Out of twelve compounds, 7b and 7d are found to be most potent of this series. The same compounds showed no neurotoxicity at the maximum dose administered (100mg/kg). Conclusions: The results obtained justify the usage of these compounds from their promising anticonvulsant activity. Further studies are needed to fully characterize the toxicity and the mechanisms involved with the anticonvulsant activity and neurotoxicity of these compounds.

Item Type:	Article
Uncontrolled Keywords:	article, male, animal experiment, animal model, controlled study, disease model, nonhuman, rat, unclassified drug, drug structure, drug synthesis, structure activity relation, 3, anticonvulsant activity, drug potency, neurotoxicity, seizure, drug effect, drug purity, in vivo study, phenytoin, anticonvulsive agent, rotarod test, 1 methyl n (5 (4 ((2 nitro 4 (trifluoromethyl)phenyl)sulfonyl)piperazin 1 yl) 1, 1 methyl n (5 (4 ((3 (trifluoromethyl)phenyl)sulfonyl)piperazin 1 yl) 1, 1 methyl n (5 (4 ((4 (trifluoromethyl)phenyl)sulfonyl)piperazin 1 yl) 1, 1 methyl n (5 (4 tosylpiperazin 1 yl) 1, 1 methyl n (naphthalen 2 ylsulfonyl) n (5 (4 (naphthalen 2 ylsulfonyl)piperazin 1 yl) 1, 4 thiadiazol 2 yl) 1 methyl 1h indazole 3 carboxamide, 4 thiadiazol 2 yl) 1h indazole 3 carboxamide, 4 thiadiazol 2 yl)methyl 1h indazole 3 carboxamide, 5 bis(trifluoromethyl)phenyl)sulfonyl)piperazin 1 yl) 1, 5 dichlorothiophen 3 yl)sulfonyl)piperazin 1 yl) 1, 5 dimethylisoxazol 4 yl)sulfonyl)piperazin 1 yl) 1, maximal electroshock seizure model, n (5 (4 ((2, n (5 (4 ((3, n (5 (4 ((4 bromophenyl)sulfonyl)piperazin 1 yl) 1, n (5 (4 ((4 cyanophenyl)sulfonyl)piperazin 1 yl) 1, n (5 (4 ((4 iodophenyl)sulfonyl)piperazin 1 yl) 1, n (5 (4 (methylsulfonyl)piperazin 1 yl) 1
Subjects:	C Chemical Science > Chemistry
Divisions:	Department of > Chemistry
Depositing User:	Arshiya Kousar Library Assistant
Date Deposited:	16 Sep 2019 05:36
Last Modified:	16 Sep 2019 05:36
URI:	http://eprints.uni-mysore.ac.in/id/eprint/8010

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