{"title":"含咪唑[2,1-b]噻唑基团的新型4-噻唑烷酮的合成及抗病毒活性评价","authors":"N. Güzeldemirci, E. Pehlivan, L. Naesens","doi":"10.12991/MPJ.2018.61","DOIUrl":null,"url":null,"abstract":"A series of new 4-thiazolidinone derivatives were synthesized and evaluated against diverse DNAand RNA-viruses in mammalian cell cultures. Some of the compounds were found to exhibit moderate antiviral activity. 3Propyl-2-[((6-(4-chlorophenyl)imidazo[2,1-b]thiazol-3-yl)acetyl)hydrazono]-5-methyl-4-thiazolidinone 13, displayed modest yet consistent activity against three strains of influenza A virus, including the 2009 pandemic virus A/H1N1 Virginia/ATCC3/2009 (cytotoxicity >100 μM). Compounds 6 and 11 displayed activity against vesicular stomatitis virus in HeLa cells (antiviral EC50 values of 9 (cytotoxicity 100 μM) and 2 μM (cytotoxicity 20 μM), respectively). Neither of the compounds was active against HIV.","PeriodicalId":18529,"journal":{"name":"Marmara Pharmaceutical Journal","volume":"6 1","pages":"237-248"},"PeriodicalIF":0.0000,"publicationDate":"2018-04-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"11","resultStr":"{\"title\":\"Synthesis and antiviral activity evaluation of new 4-thiazolidinones bearing an imidazo[2,1-b]thiazole moiety\",\"authors\":\"N. Güzeldemirci, E. Pehlivan, L. Naesens\",\"doi\":\"10.12991/MPJ.2018.61\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"A series of new 4-thiazolidinone derivatives were synthesized and evaluated against diverse DNAand RNA-viruses in mammalian cell cultures. Some of the compounds were found to exhibit moderate antiviral activity. 3Propyl-2-[((6-(4-chlorophenyl)imidazo[2,1-b]thiazol-3-yl)acetyl)hydrazono]-5-methyl-4-thiazolidinone 13, displayed modest yet consistent activity against three strains of influenza A virus, including the 2009 pandemic virus A/H1N1 Virginia/ATCC3/2009 (cytotoxicity >100 μM). Compounds 6 and 11 displayed activity against vesicular stomatitis virus in HeLa cells (antiviral EC50 values of 9 (cytotoxicity 100 μM) and 2 μM (cytotoxicity 20 μM), respectively). Neither of the compounds was active against HIV.\",\"PeriodicalId\":18529,\"journal\":{\"name\":\"Marmara Pharmaceutical Journal\",\"volume\":\"6 1\",\"pages\":\"237-248\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2018-04-06\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"11\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Marmara Pharmaceutical Journal\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.12991/MPJ.2018.61\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Marmara Pharmaceutical Journal","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.12991/MPJ.2018.61","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Synthesis and antiviral activity evaluation of new 4-thiazolidinones bearing an imidazo[2,1-b]thiazole moiety
A series of new 4-thiazolidinone derivatives were synthesized and evaluated against diverse DNAand RNA-viruses in mammalian cell cultures. Some of the compounds were found to exhibit moderate antiviral activity. 3Propyl-2-[((6-(4-chlorophenyl)imidazo[2,1-b]thiazol-3-yl)acetyl)hydrazono]-5-methyl-4-thiazolidinone 13, displayed modest yet consistent activity against three strains of influenza A virus, including the 2009 pandemic virus A/H1N1 Virginia/ATCC3/2009 (cytotoxicity >100 μM). Compounds 6 and 11 displayed activity against vesicular stomatitis virus in HeLa cells (antiviral EC50 values of 9 (cytotoxicity 100 μM) and 2 μM (cytotoxicity 20 μM), respectively). Neither of the compounds was active against HIV.