{"title":"[3-喹啉吡啶-1′-酰基-5- r -吲哚的合成及药理活性]。","authors":"C Boido-Canu, V Boido, F Sparatore, A Sparatore","doi":"","DOIUrl":null,"url":null,"abstract":"<p><p>By acid action on the mixture of homolupinal diethylacetal and arylhydrazines several 3-quinolizidin-1'-yl-5-R-indoles (III a - III e) were prepared. The homolupinal diethylacetal, whose hydrolysis gives rise to the unknown aldehyde, was obtained through the action of lupinylmagnesium chloride on diethylphenylorthoformate. Compounds (III) were subjected to wide pharmacological screening; all of them exhibited calcium blocking, negative cardioinotropic and diuretic activities, while single compounds showed antiinflammatory (III d), anticonvulsant and hypoglycemic (III e) activities.</p>","PeriodicalId":13279,"journal":{"name":"Il Farmaco; edizione scientifica","volume":"43 10","pages":"801-17"},"PeriodicalIF":0.0000,"publicationDate":"1988-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"[Synthesis and pharmacologic activity of 3-quinolizidine-1'-yl-5-R-indoles].\",\"authors\":\"C Boido-Canu, V Boido, F Sparatore, A Sparatore\",\"doi\":\"\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>By acid action on the mixture of homolupinal diethylacetal and arylhydrazines several 3-quinolizidin-1'-yl-5-R-indoles (III a - III e) were prepared. The homolupinal diethylacetal, whose hydrolysis gives rise to the unknown aldehyde, was obtained through the action of lupinylmagnesium chloride on diethylphenylorthoformate. Compounds (III) were subjected to wide pharmacological screening; all of them exhibited calcium blocking, negative cardioinotropic and diuretic activities, while single compounds showed antiinflammatory (III d), anticonvulsant and hypoglycemic (III e) activities.</p>\",\"PeriodicalId\":13279,\"journal\":{\"name\":\"Il Farmaco; edizione scientifica\",\"volume\":\"43 10\",\"pages\":\"801-17\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1988-10-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Il Farmaco; edizione scientifica\",\"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":"Il Farmaco; edizione scientifica","FirstCategoryId":"1085","ListUrlMain":"","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0
摘要
通过对同醇缩二乙基缩醛和芳基肼的酸作用,制备了几种3-喹啉吡啶-1′-酰基-5- r -吲哚(III a - III e)。通过羽豆酰氯镁对苯基甲酸二乙酯的作用,得到了同醇缩二乙缩醛,其水解生成未知的醛。化合物(III)经过广泛的药理学筛选;所有化合物均表现出钙阻滞、负性促心和利尿活性,而单一化合物表现出抗炎(III d)、抗惊厥和降血糖(III e)活性。
[Synthesis and pharmacologic activity of 3-quinolizidine-1'-yl-5-R-indoles].
By acid action on the mixture of homolupinal diethylacetal and arylhydrazines several 3-quinolizidin-1'-yl-5-R-indoles (III a - III e) were prepared. The homolupinal diethylacetal, whose hydrolysis gives rise to the unknown aldehyde, was obtained through the action of lupinylmagnesium chloride on diethylphenylorthoformate. Compounds (III) were subjected to wide pharmacological screening; all of them exhibited calcium blocking, negative cardioinotropic and diuretic activities, while single compounds showed antiinflammatory (III d), anticonvulsant and hypoglycemic (III e) activities.