Synthesis and CNS activity of new 1-alkyl-2-aryl-7-hydroxy-5(1H)oxo-imidazo[1,2-a]pyrymidines.
Cyclocondensation of 1,5-disubstituted 2-aminoimidazolines with diethyl malonate in the presence of sodium methanolate leading to imidazol[1,2-alpyrimidine-5,7-dion system is presented. Prevailing of 7-hydroxy-5(1H)oxo form between three possible tautomers is discussed based on spectral data. CNS activity of nine compounds is evaluated.
Matosiuk
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Department of Medicines Technology, Faculty of Pharmacy, School of Medicine, Lublin, Poland.
Tkaczyński
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T
Stefańczyk
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D000818:Animals; D001058:Apomorphine / Q000633:toxicity; D002375:Catalepsy / Q000139:chemically induced / Q000188:drug therapy; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D006220:Haloperidol / Q000633:toxicity; D007035:Hypothermia / Q000139:chemically induced / Q000188:drug therapy; D007928:Lethal Dose 50; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D008314:Malonates / Q000737:chemistry; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D010146:Pain / Q000188:drug therapy; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D051381:Rats; D017208:Rats, Wistar; D012110:Reserpine / Q000633:toxicity; D012640:Seizures / Q000188:drug therapy; D012890:Sleep / Q000187:drug effects; D013239:Stereotyped Behavior / Q000187:drug effects; D013329:Structure-Activity Relationship
D008314:Malonates; D011743:Pyrimidines; D012110:Reserpine; D006220:Haloperidol; D001058:Apomorphine; C030978:diethylmalonic acid