1: Epilepsia 1997 Mar;38(3):334-7
Anticonvulsant activity of pyrid-3-yl-sulfonyl ureas and thioureas.
Masereel B, Lambert DM, Dogne JM, Poupaert JH, Delarge J
Department of Medicinal Chemistry, Institute of Pharmacy, University of
Liege, Belgium.
The N-[(4-cycloheptylaminopyrid-3-yl)sulfonyl]-N'-cycloheptyl urea, a neuroprotective
agent, and 10 chemically related sulfonyl(thio)ureas were evaluated in
the maximal electroshock seizure test in mice. This sulfonylurea, BM 27,
and two structurally related sulfonylthioureas, BM 11 and BM 34, emerged
with a 50% effective dose (ED50) of 2.87, 1.72, and 1.19 mg/kg, respectively.
Their anticonvulsant profiles were found to be similar to that of phenytoin:
active in the maximal electroshock seizure (MES) test and inactive in chemically
induced seizures (pentetrazole, strychnine, bicuculline, picrotoxine,N-methyl-D,L-aspartic
acid). These compounds exhibited a higher protective index and potency
than those of phenytoin. Additional work remains necessary, however, to
determine whether BM 27 is of clinical interest.
PMID: 9070596, UI: 97224015