2-Pyrrolidinylideneureas, a new class of central nervous system agents.
A series of N-aryl-N'-(1-methyl-2-pyrrolidinylidene)ureas was prepared and screened for pharmacological activity. Congeners possessing either phenyl or phenyl substituted with 4-nitro, 3-bromo, 3-chloro, 3-fluoro, and 3-methyl groups were found to demonstrate anxiolytic activity. 2,6-Disubstitution of the phenyl ring with methyl, chloro, and bromo imparted potent muscle-relaxant properties which appear to be centrally mediated. A significant separation of the anxiolytic and muscle-relaxant properties from other CNS activities, e.g., anticonvulsant, sedative, and hypnotic, was achieved.
D000818:Animals; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis; D000927:Anticonvulsants / Q000138:chemical synthesis; D002491:Central Nervous System Agents / Q000138:chemical synthesis*; D004305:Dose-Response Relationship, Drug; D006993:Hypnotics and Sedatives / Q000138:chemical synthesis; D007928:Lethal Dose 50; D051379:Mice; D009125:Muscle Relaxants, Central / Q000138:chemical synthesis; D011759:Pyrrolidines / Q000138:chemical synthesis / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship; D013890:Thiourea / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology; D014508:Urea / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
D014151:Anti-Anxiety Agents; D000927:Anticonvulsants; D002491:Central Nervous System Agents; D006993:Hypnotics and Sedatives; D009125:Muscle Relaxants, Central; D011759:Pyrrolidines; D014508:Urea; D013890:Thiourea