Abstract
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.
MeSH terms
-
Animals
-
Apomorphine / toxicity
-
Catalepsy / chemically induced
-
Catalepsy / drug therapy
-
Drug Design
-
Drug Evaluation, Preclinical
-
Haloperidol / toxicity
-
Hypothermia / chemically induced
-
Hypothermia / drug therapy
-
Lethal Dose 50
-
Magnetic Resonance Spectroscopy
-
Male
-
Malonates / chemistry
-
Mice
-
Motor Activity / drug effects
-
Pain / drug therapy
-
Pyrimidines / chemical synthesis*
-
Pyrimidines / pharmacology
-
Pyrimidines / therapeutic use
-
Rats
-
Rats, Wistar
-
Reserpine / toxicity
-
Seizures / drug therapy
-
Sleep / drug effects
-
Stereotyped Behavior / drug effects
-
Structure-Activity Relationship
Substances
-
Malonates
-
Pyrimidines
-
Reserpine
-
Haloperidol
-
Apomorphine
-
diethylmalonic acid