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Molecules 2015, 20(9), 17585-17600;

Synthesis and Pharmacological Evaluation of Novel Benzenesulfonamide Derivatives as Potential Anticonvulsant Agents

State Key Laboratory of Virology, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Ministry of Education, Wuhan University School of Pharmaceutical Sciences, 185 Donghu Road, Wuhan 430071, China
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editor: Maria Emília de Sousa
Received: 30 July 2015 / Revised: 17 September 2015 / Accepted: 17 September 2015 / Published: 23 September 2015
(This article belongs to the Section Medicinal Chemistry)
Full-Text   |   PDF [733 KB, uploaded 23 September 2015]   |  


A novel series of benzenesulfonamide derivatives containing 4-aminobenzenesul-fonamide and α-amides branched valproic acid or 2,2-dimethylcyclopropanecarboxylic acid moieties were synthesized and screened for their anticonvulsant activities in mice maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) test. The activity experimental study showed that 2,2-dipropyl-N1-(4-sulfamoylphenyl)malonamide (18b) had the lowest median effective dose (ED50) of 16.36 mg/kg in MES test, and 2,2-dimethyl-N-(4-sulfamoylphenyl)cyclopropane-1,1-dicarboxamide (12c) had the lowest ED50 of 22.50 mg/kg in scPTZ test, which resulted in the protective indexe (PI) of 24.8 and 20.4, respectively. These promising data suggest the new compounds have good potential as new class of anticonvulsant agents with high effectiveness and low toxicity for the treatment of epilepsy. View Full-Text
Keywords: sulfonamide; anticonvulsant; MES; scPTZ sulfonamide; anticonvulsant; MES; scPTZ

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Wang, Z.; Li, J.; Zeng, X.-D.; Hu, X.-M.; Zhou, X.; Hong, X. Synthesis and Pharmacological Evaluation of Novel Benzenesulfonamide Derivatives as Potential Anticonvulsant Agents. Molecules 2015, 20, 17585-17600.

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