ANTICONVULSANT ACTIVITY OF PYRID-3-YL-SULFONYL UREAS AND THIOUREAS

The ycloheptylaminopyrid-3-yl)sulfonyl]-N'-cycloheptyl urea, a neuropr otective agent, and 10 chemically related sulfonyl(thio)ureas were eva luated in the maximal electroshock seizure test in mice. This sulfonyl urea, BM 27, and two structurally related sulfonylthioureas, BM 11 and BM 34, emerged with a 50% effective dose (ED(50)) 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 se izure (MES) test and inactive in chemically induced seizures (pentetra zole, strychnine, bicuculline, picrotoxine, N-methyl-D,L-aspartic acid ). These compounds exhibited a higher protective index and potency tha n those of phenytoin. Additional work remains necessary, however, to d etermine whether BM 27 is of clinical interest.