Synthesis and some central pharmacological properties of new derivatives of 2,3-dihydroimidazo[1,2-a]pyrimidine-6-carboxylic acid.

D Matosiuk, T Tkaczyński, E Jagiełło-Wójtowicz, I Zebrowska-Lupina, S J Czuczwar, B Matuszek, B Klenk-Majewska, Z Danilczuk, W Janusz, Z Kleinrok
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Abstract

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.

2,3-二氢咪唑[1,2-a]嘧啶-6-羧酸新衍生物的合成及一些主要药理性质
得到了21个芳香环位于1或2位的2,3-二氢咪唑[1,2-a]嘧啶-6-羧酸衍生物(6个正丁基酰胺和15个游离酸)。它们是由各自的乙酯通过氨解或水解合成的。对化合物1、2、4、5、7、8、9和10的中心作用进行了小鼠和大鼠的药理研究。最活跃的化合物,产生镇静和低温,还有1 2和5。这些化合物降低了安非他明引起的多动症。此外,化合物2对小鼠也有镇痛作用。
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