Synthesis and some central pharmacological properties of new derivatives of 2,3-dihydroimidazo[1,2-a]pyrimidine-6-carboxylic acid.
Twenty one derivatives of 2,3-dihydroimidazo[1,2-a]pyrimidine-6-carboxylic acid (6 n-butyl amides and 15 free acids) bearing the aromatic ring in position 1 or 2 were obtained. They were synthesized by aminolysis or hydrolysis of respective ethyl esters. Pharmacological studies on the central action of eight compounds 1, 2, 4, 5, 7, 8, 9 and 10 were carried out on mice and rats. The most active compounds, producing sedation and hypothermia, and 1, 2 and 5. The compounds decreased amphetamine-induced hyperactivity. Besides, compound 2 exerted analgesic effect in mice.
Matosiuk
D
D
Department of Chemical Technology of Drugs, Medical Academy, Lublin, Poland.
Tkaczyński
T
T
Jagiełło-Wójtowicz
E
E
Zebrowska-Lupina
I
I
Czuczwar
S J
SJ
Matuszek
B
B
Klenk-Majewska
B
B
Danilczuk
Z
Z
Janusz
W
W
Kleinrok
Z
Z
D000818:Animals; D001831:Body Temperature / Q000187:drug effects; D001921:Brain / Q000187:drug effects* / Q000503:physiopathology; D003080:Cold Temperature; D004597:Electroshock; D007093:Imidazoles / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D010146:Pain / Q000188:drug therapy; D011743:Pyrimidines / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D051381:Rats; D017208:Rats, Wistar
D007093:Imidazoles; D011743:Pyrimidines