F. Somers, P. Tullio, S. Boverie, J. Dogné, X. Leval, M. Antoine, P. Lebrun, B. Pirotte
{"title":"新型3-烷基氨基- 4h -1,2,4-苯并噻嗪1,1-二氧化物的合成及其对胰岛素分泌细胞的生物学效应","authors":"F. Somers, P. Tullio, S. Boverie, J. Dogné, X. Leval, M. Antoine, P. Lebrun, B. Pirotte","doi":"10.1211/096089296765556980","DOIUrl":null,"url":null,"abstract":"3-Alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides with nitro, amino or acetylamino groups in the 7-position have been synthesized in an attempt to discover new tissue-selective KATP-channel openers. \n \nThe compounds were tested as putative pancreatic β-cells KATP-channel openers by measuring their inhibitory activity on the insulin releasing process. The influence of the substituent in the 7-position on the acidic character (pKa) and on biological activity is discussed. \n \nThe nitrobenzene derivatives were biologically active, but less so than the un-derivatized parent pyridothiadiazine dioxides.","PeriodicalId":19946,"journal":{"name":"Pharmacy and Pharmacology Communications","volume":"10 1","pages":"89-95"},"PeriodicalIF":0.0000,"publicationDate":"2000-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"2","resultStr":"{\"title\":\"Synthesis and biological effects of new 3-alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides on insulin-secreting cells\",\"authors\":\"F. Somers, P. Tullio, S. Boverie, J. Dogné, X. Leval, M. Antoine, P. Lebrun, B. Pirotte\",\"doi\":\"10.1211/096089296765556980\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"3-Alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides with nitro, amino or acetylamino groups in the 7-position have been synthesized in an attempt to discover new tissue-selective KATP-channel openers. \\n \\nThe compounds were tested as putative pancreatic β-cells KATP-channel openers by measuring their inhibitory activity on the insulin releasing process. The influence of the substituent in the 7-position on the acidic character (pKa) and on biological activity is discussed. \\n \\nThe nitrobenzene derivatives were biologically active, but less so than the un-derivatized parent pyridothiadiazine dioxides.\",\"PeriodicalId\":19946,\"journal\":{\"name\":\"Pharmacy and Pharmacology Communications\",\"volume\":\"10 1\",\"pages\":\"89-95\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2000-02-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"2\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Pharmacy and Pharmacology Communications\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1211/096089296765556980\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Pharmacy and Pharmacology Communications","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1211/096089296765556980","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Synthesis and biological effects of new 3-alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides on insulin-secreting cells
3-Alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides with nitro, amino or acetylamino groups in the 7-position have been synthesized in an attempt to discover new tissue-selective KATP-channel openers.
The compounds were tested as putative pancreatic β-cells KATP-channel openers by measuring their inhibitory activity on the insulin releasing process. The influence of the substituent in the 7-position on the acidic character (pKa) and on biological activity is discussed.
The nitrobenzene derivatives were biologically active, but less so than the un-derivatized parent pyridothiadiazine dioxides.
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