Abstract
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.
Highlights
Epilepsy is a common neurological disorder that affects approximately 50 million people around the world [1,2,3]
We introduced amid groups to the benzenesulfonamide system in order to get novel anticonvulsant agents
A series of benzenesulfonamide derivatives containing 4-aminobenzenesulfonamide and α-amides branched valproic acid or 2,2-dimethylcyclopropanecarboxylic acid moieties were synthesized and their pharmacological activities as potential anticonvulsant agents were evaluated in mice maximal maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole tests in this paper
Summary
Epilepsy is a common neurological disorder that affects approximately 50 million people around the world [1,2,3]. In 2008, Jakob reported the synthesis and high potency of TMCD-benzenesulfonamide (3, ED50 = 26 mg/kg) along with a wide protective index (PI = TD50/ED50 >19) in the rat-MES test [19]. It was reported that α-fluoronated TMCD (4) was 120 times more potent than VPA in the rat-scMet test (ED50 = 6 mg/kg) with a remarkable protective index (PI = 20) [20]. These developments prompted us to focus on systematic structural modifications in the α position. A series of benzenesulfonamide derivatives containing 4-aminobenzenesulfonamide and α-amides branched valproic acid or 2,2-dimethylcyclopropanecarboxylic acid moieties were synthesized and their pharmacological activities as potential anticonvulsant agents were evaluated in mice maximal MES and subcutaneous pentylenetetrazole (scPTZ) tests in this paper
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