D Matosiuk, T Tkaczyński, E Jagiełło-Wójtowicz, I Zebrowska-Lupina, S J Czuczwar, B Matuszek, B Klenk-Majewska, Z Danilczuk, W Janusz, Z Kleinrok
{"title":"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","authors":"D Matosiuk, T Tkaczyński, E Jagiełło-Wójtowicz, I Zebrowska-Lupina, S J Czuczwar, B Matuszek, B Klenk-Majewska, Z Danilczuk, W Janusz, Z Kleinrok","doi":"","DOIUrl":null,"url":null,"abstract":"<p><p>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.</p>","PeriodicalId":20276,"journal":{"name":"Polish journal of pharmacology and pharmacy","volume":"44 1","pages":"67-78"},"PeriodicalIF":0.0000,"publicationDate":"1992-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis and some central pharmacological properties of new derivatives of 2,3-dihydroimidazo[1,2-a]pyrimidine-6-carboxylic acid.\",\"authors\":\"D Matosiuk, T Tkaczyński, E Jagiełło-Wójtowicz, I Zebrowska-Lupina, S J Czuczwar, B Matuszek, B Klenk-Majewska, Z Danilczuk, W Janusz, Z Kleinrok\",\"doi\":\"\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>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.</p>\",\"PeriodicalId\":20276,\"journal\":{\"name\":\"Polish journal of pharmacology and pharmacy\",\"volume\":\"44 1\",\"pages\":\"67-78\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1992-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Polish journal of pharmacology and pharmacy\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Polish journal of pharmacology and pharmacy","FirstCategoryId":"1085","ListUrlMain":"","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
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.