title: Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 4. Amidines.
abstract: Two different structural types of 2-aryl-1,3,4-thiadiazole amidines were synthesized and evaluated for anticonvulsant activity. Enhancement of the inherent anticonvulsant activity therein and separation of this activity from the accompanying sedative action of these compounds were attempted. The most potent compounds occurred in the 2-(trifluoromethyl)phenyl series of type 3 amidines, but they also possessed a relatively high level of neurotoxicity and sedation as demonstrated in the rotorod test.
authors.affiliation: Department of Medicinal Chemistry, Reckitt and Colman plc, Kingston-upon-Hull, United Kingdom.
authors.forename: C B
authors.initials: CB
authors.lastname: Chapleo
authors.forename: P L
authors.initials: PL
authors.lastname: Myers
authors.forename: A C
authors.initials: AC
authors.lastname: Smith
authors.forename: M R
authors.initials: MR
authors.lastname: Stillings
authors.forename: I F
authors.initials: IF
authors.lastname: Tulloch
authors.forename: D S
authors.initials: DS
authors.lastname: Walter
mesh_terms: D000578:Amidines / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis*; D004597:Electroshock; D007202:Indicators and Reagents; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D010433:Pentylenetetrazole; D012640:Seizures / Q000503:physiopathology; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000578:Amidines; D000927:Anticonvulsants; D007202:Indicators and Reagents; D013830:Thiadiazoles; D010433:Pentylenetetrazole