L Ignatovich, D Zarina, I Shestakova, S Germane, E Lukevics
{"title":"硅基和菌基取代三氟乙酰呋喃的合成及其生物活性。","authors":"L Ignatovich, D Zarina, I Shestakova, S Germane, E Lukevics","doi":"10.1155/MBD.2001.211","DOIUrl":null,"url":null,"abstract":"<p><p>A series of silyl, germyl and alkyl substituted trifluoroacetylfurans has been synthesized under Friedel-Crafts electrophilic acylation conditions. Biological investigations have demonstrated that germyl derivatives of trifluoroacetylfuran are more toxic than the silicon analogues. 5-Triethylgermyl-2- trifluoroacetylfuran was the most toxic compound (CD(nabla), 11.2 mg kg(-1), i.p. for white mice), 200 times more toxic than the silicon analogue. 5-t-Butyl- and 5-trimethylsilyl-2-trifluroacetylfuran prolong the duration of ethanol anaesthesia by 220 and 140%. 5-Triethylgermyl-2-trifluroacetylfuran exibited high anesthetic activity in hexobarbital test (prolonged the duration by 137%). Some of compounds influenced muscle tone and locomotor coordination parameters. 5-Triethylgermyl-2-trifluomacetylfuran exibited analgesic activity (D(nabla), 0.9 mg k}(-infinity)).</p>","PeriodicalId":18452,"journal":{"name":"Metal-Based Drugs","volume":"8 4","pages":"211-4"},"PeriodicalIF":0.0000,"publicationDate":"2001-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1155/MBD.2001.211","citationCount":"12","resultStr":"{\"title\":\"Synthesis and biological activity of silyl- and germylsubstituted trifluroacetylfurans.\",\"authors\":\"L Ignatovich, D Zarina, I Shestakova, S Germane, E Lukevics\",\"doi\":\"10.1155/MBD.2001.211\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>A series of silyl, germyl and alkyl substituted trifluoroacetylfurans has been synthesized under Friedel-Crafts electrophilic acylation conditions. Biological investigations have demonstrated that germyl derivatives of trifluoroacetylfuran are more toxic than the silicon analogues. 5-Triethylgermyl-2- trifluoroacetylfuran was the most toxic compound (CD(nabla), 11.2 mg kg(-1), i.p. for white mice), 200 times more toxic than the silicon analogue. 5-t-Butyl- and 5-trimethylsilyl-2-trifluroacetylfuran prolong the duration of ethanol anaesthesia by 220 and 140%. 5-Triethylgermyl-2-trifluroacetylfuran exibited high anesthetic activity in hexobarbital test (prolonged the duration by 137%). Some of compounds influenced muscle tone and locomotor coordination parameters. 5-Triethylgermyl-2-trifluomacetylfuran exibited analgesic activity (D(nabla), 0.9 mg k}(-infinity)).</p>\",\"PeriodicalId\":18452,\"journal\":{\"name\":\"Metal-Based Drugs\",\"volume\":\"8 4\",\"pages\":\"211-4\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2001-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1155/MBD.2001.211\",\"citationCount\":\"12\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Metal-Based Drugs\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1155/MBD.2001.211\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Metal-Based Drugs","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1155/MBD.2001.211","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Synthesis and biological activity of silyl- and germylsubstituted trifluroacetylfurans.
A series of silyl, germyl and alkyl substituted trifluoroacetylfurans has been synthesized under Friedel-Crafts electrophilic acylation conditions. Biological investigations have demonstrated that germyl derivatives of trifluoroacetylfuran are more toxic than the silicon analogues. 5-Triethylgermyl-2- trifluoroacetylfuran was the most toxic compound (CD(nabla), 11.2 mg kg(-1), i.p. for white mice), 200 times more toxic than the silicon analogue. 5-t-Butyl- and 5-trimethylsilyl-2-trifluroacetylfuran prolong the duration of ethanol anaesthesia by 220 and 140%. 5-Triethylgermyl-2-trifluroacetylfuran exibited high anesthetic activity in hexobarbital test (prolonged the duration by 137%). Some of compounds influenced muscle tone and locomotor coordination parameters. 5-Triethylgermyl-2-trifluomacetylfuran exibited analgesic activity (D(nabla), 0.9 mg k}(-infinity)).