Design, synthesis, and anticonvulsant activity of 1-(pyrid-3-ylsulfonamido)-2-nitroethylenes

B Masereel, J Wouters, L Pochet…

Index: Masereel, Bernard; Wouters, Johan; Pochet, Lionel; Lambert, Didier Journal of Medicinal Chemistry, 1998 , vol. 41, # 17 p. 3239 - 3244

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Citation Number: 17

Abstract

The lipophilic 1-cycloalkylamino-1-(pyrid-3-yl-sulfonamido)-2-nitroethylenes were synthesized as bioisosteres of BM-34, an anticonvulsant sulfonylthiourea. Compound 17 (ip) emerged from the maximal electroshock seizure (MES) test with a 50% effective dose (ED50) of 8.25 mg/kg. Its anticonvulsant profile was similar to that of phenytoin (ED50= 9.51 mg/kg) and of BM-34 (ED50= 1.19 mg/kg): active in the MES test and inactive in seizures ...