Synthesis and anticonvulsant activity of some new hexahydropyrimidine-2,4-dione derivatives.
In this study, twelve new hexahydropyrimidine-2,4-dione derivatives were synthesized and screened for their anticonvulsant activities. All the compounds (7a-1) which have 6-arylhexahydropyrimidine-2,4-dione and N,N-disubstituted dithiocarbamate structures were prepared by the reaction with appropriate 3-(2-chloroethyl)-6-arylhexahydropyrimidine-2,4diones and the corresponding N,N-disubstituted dithiocarbamate potassium salts. The structure of the synthesized compounds was confirmed by UV, IR, 1H-NMR and elemental analysis. Their anticonvulsant activities were determined by maximal electroshock (MES), subcutaneous pentetrazol (metrazol, scMet) and rotorod toxicity tests for neurological deficits. According to the activity studies, 6-(4-chlorophenyl)hexahydropyrimidine-2,4-dione derivatives (7e-h) were found to be highly protective against MES and scMet. Neurotoxicity was not observed in any of the tested compounds.
Septioglu
Ebubekir
E
Hacettepe University, Faculty of Pharmacy, Pharmaceutical Chemistry Department, Ankara, Turkey.
Aytemir
Mutlu Dilsiz
MD
Caliş
Unsal
U
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology*; D003292:Convulsants; D004597:Electroshock; D007202:Indicators and Reagents; D007274:Injections, Intraperitoneal; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D020258:Neurotoxicity Syndromes / Q000523:psychology; D010433:Pentylenetetrazole; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D012640:Seizures / Q000139:chemically induced / Q000517:prevention & control; D013055:Spectrophotometry, Infrared; D013056:Spectrophotometry, Ultraviolet; D013329:Structure-Activity Relationship
D000927:Anticonvulsants; D003292:Convulsants; D007202:Indicators and Reagents; D011743:Pyrimidines; C502309:hexahydropyrimidine-2,4-dione; D010433:Pentylenetetrazole