Matosiuk D, Tkaczyński T, Jagiełło-Wójtowicz E, Zebrowska-Lupina I, Czuczwar S J, Matuszek B, Klenk-Majewska B, Danilczuk Z, Janusz W, Kleinrok Z
Department of Chemical Technology of Drugs, Medical Academy, Lublin, Poland.
Pol J Pharmacol Pharm. 1992 Jan-Feb;44(1):67-78.
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.
获得了21种在1位或2位带有芳环的2,3-二氢咪唑并[1,2-a]嘧啶-6-羧酸衍生物(6种正丁酰胺和15种游离酸)。它们通过相应乙酯的氨解或水解反应合成。对8种化合物1、2、4、5、7、8、9和10的中枢作用进行了小鼠和大鼠的药理学研究。活性最强的化合物可产生镇静和体温过低作用,分别为1、2和5。这些化合物可降低苯丙胺引起的多动。此外,化合物2对小鼠具有镇痛作用。