Anticonvulsant 4-aryl semicarbazides & thioureas

Abstract

Among a series of anticonvulsant 1-aryl semicarbazides, 1-(3-5-bistrifluoromethyl)phenylsemicarbazide, C3884-Go(11) and its 4-methyl derivative, C 3165-Go (12) showed good activity of long duration in the electroshock test in mice and rats. Quantitative structure activity analysis indicates that c and n values are respectively important for the aromatic and side chain substituents respectively. N-Acetyl-N'-(3,5-bistrifiuoromethyl)phenyl hydrazine (20) is highly anticonvulsant but causes ataxia. 4-Aryl thiosemicarbazides show weak to moderate activity. Among N-(3,5-bistrifluoromethyl)phenyl thiocarbamoyl derivatives, the product 33 from N-benzyl piperazine is potent in the electroshock' test. Compounds 11 and 12 have been compared with standards such as phenytoin, phenurone and carbamazepine.