{"title":"多元咪唑[2,1-b][1,3]噻嗪类化合物的合成及非甾体抗炎剂的评价","authors":"N. Slyvka, S. Holota, L. Saliyeva, M. Vovk","doi":"10.3390/ecsoc-25-11692","DOIUrl":null,"url":null,"abstract":": The present work is devoted to the synthesis of imidazo[2,1- b ][1,3]thiazine derivatives as possible anti-inflammatory agents. The synthetic approach to (2-pyridinyloxy)substituted imid-azo[2,1- b ][1,3]thiazines based on the interaction of the polysubstituted 2-chloropyridines with 3-hydroxy-imidazo[2,1- b ][1,3]thiazines was proposed. Selective nucleophilic substitution in position 2 of pyridine ring was observed in the mentioned reaction. The synthesized (2-pyridinyloxy)substi-tuted imidazo[2,1- b ][1,3]thiazines drug-like properties were studied in silico using SwissADME and anti-inflammatory activity in carrageenan test in vivo. Hit-compounds with satisfactory drug-like and pharmacological features were identified as promising objects for futhercoming structure opti-mization and in-depth studies.","PeriodicalId":11441,"journal":{"name":"ECSOC-25","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2021-11-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthetic Approach to Diversified Imidazo[2,1-b][1,3]thiazines and Its Evaluation as Non-Steroidal Anti-Inflammatory Agents †\",\"authors\":\"N. Slyvka, S. Holota, L. Saliyeva, M. Vovk\",\"doi\":\"10.3390/ecsoc-25-11692\",\"DOIUrl\":null,\"url\":null,\"abstract\":\": The present work is devoted to the synthesis of imidazo[2,1- b ][1,3]thiazine derivatives as possible anti-inflammatory agents. The synthetic approach to (2-pyridinyloxy)substituted imid-azo[2,1- b ][1,3]thiazines based on the interaction of the polysubstituted 2-chloropyridines with 3-hydroxy-imidazo[2,1- b ][1,3]thiazines was proposed. Selective nucleophilic substitution in position 2 of pyridine ring was observed in the mentioned reaction. The synthesized (2-pyridinyloxy)substi-tuted imidazo[2,1- b ][1,3]thiazines drug-like properties were studied in silico using SwissADME and anti-inflammatory activity in carrageenan test in vivo. Hit-compounds with satisfactory drug-like and pharmacological features were identified as promising objects for futhercoming structure opti-mization and in-depth studies.\",\"PeriodicalId\":11441,\"journal\":{\"name\":\"ECSOC-25\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2021-11-14\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"ECSOC-25\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.3390/ecsoc-25-11692\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"ECSOC-25","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.3390/ecsoc-25-11692","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Synthetic Approach to Diversified Imidazo[2,1-b][1,3]thiazines and Its Evaluation as Non-Steroidal Anti-Inflammatory Agents †
: The present work is devoted to the synthesis of imidazo[2,1- b ][1,3]thiazine derivatives as possible anti-inflammatory agents. The synthetic approach to (2-pyridinyloxy)substituted imid-azo[2,1- b ][1,3]thiazines based on the interaction of the polysubstituted 2-chloropyridines with 3-hydroxy-imidazo[2,1- b ][1,3]thiazines was proposed. Selective nucleophilic substitution in position 2 of pyridine ring was observed in the mentioned reaction. The synthesized (2-pyridinyloxy)substi-tuted imidazo[2,1- b ][1,3]thiazines drug-like properties were studied in silico using SwissADME and anti-inflammatory activity in carrageenan test in vivo. Hit-compounds with satisfactory drug-like and pharmacological features were identified as promising objects for futhercoming structure opti-mization and in-depth studies.