Vaijinath A. Verma, A. R. Saundane, Rajkumar S. Meti
{"title":"席夫碱吲哚-1,3,4-恶二唑、噻唑烷酮和氮杂二酮高效抗菌、抗氧化、抗结核和抗癌药物的合成","authors":"Vaijinath A. Verma, A. R. Saundane, Rajkumar S. Meti","doi":"10.14233/AJOMC.2019.AJOMC-P175","DOIUrl":null,"url":null,"abstract":"The present investigation was under-taken to synthesize the Schiff base indole derivatives bearing of 1,3,4-oxadiazole thiazolidinone and azetidinone moieties. New series of 5-(5-substituted-3-phenyl-1H-indol-2-yl)-N-[(5-substituted-2-phenyl-1H-indol-3-yl)methylene]-1,3,4-oxadiazol-2-amines and screened their biological activities. Compound 4a showed excellent antibacterial and radical scavenging activities. Compound 5a revealed efficient to antifungal activity. In addition, compound 4a was found to be most active against H37Rv strain Mycobacterium tuberculosis. In case of anticancer activity methoxy compounds 4e and 6e against all the three tumor cell lines manifested remarkable cytotoxic activity. Compounds 4e, 5e and 6e have shown strong ferrous ions (Fe3+) reducing antioxidant power (FRAP) among the compounds screened. Compound 5b showed more potent of metal chelating on Fe2+ ions activity at all concentrations.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"163 1","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis of Schiff Base Indolyl-1,3,4-Oxadiazole, Thiazolidinone and Azetidinone as Efficient Antimicrobial, Antioxidant, Antituberculosis and Anticancer Agents\",\"authors\":\"Vaijinath A. Verma, A. R. Saundane, Rajkumar S. Meti\",\"doi\":\"10.14233/AJOMC.2019.AJOMC-P175\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"The present investigation was under-taken to synthesize the Schiff base indole derivatives bearing of 1,3,4-oxadiazole thiazolidinone and azetidinone moieties. New series of 5-(5-substituted-3-phenyl-1H-indol-2-yl)-N-[(5-substituted-2-phenyl-1H-indol-3-yl)methylene]-1,3,4-oxadiazol-2-amines and screened their biological activities. Compound 4a showed excellent antibacterial and radical scavenging activities. Compound 5a revealed efficient to antifungal activity. In addition, compound 4a was found to be most active against H37Rv strain Mycobacterium tuberculosis. In case of anticancer activity methoxy compounds 4e and 6e against all the three tumor cell lines manifested remarkable cytotoxic activity. Compounds 4e, 5e and 6e have shown strong ferrous ions (Fe3+) reducing antioxidant power (FRAP) among the compounds screened. Compound 5b showed more potent of metal chelating on Fe2+ ions activity at all concentrations.\",\"PeriodicalId\":8846,\"journal\":{\"name\":\"Asian Journal of Organic & Medicinal Chemistry\",\"volume\":\"163 1\",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2019-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Asian Journal of Organic & Medicinal Chemistry\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.14233/AJOMC.2019.AJOMC-P175\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Asian Journal of Organic & Medicinal Chemistry","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.14233/AJOMC.2019.AJOMC-P175","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
本文研究了含1,3,4-恶二唑噻唑烷酮和氮杂二酮的希夫碱吲哚衍生物的合成。新系列5-(5-取代-3-苯基- 1h -吲哚-2-基)- n -[(5-取代-2-苯基- 1h -吲哚-3-基)亚甲基]-1,3,4-恶二唑-2胺并筛选其生物活性。化合物4a具有良好的抗菌和自由基清除活性。化合物5a具有良好的抗真菌活性。此外,化合物4a对H37Rv结核分枝杆菌最有效。在抗肿瘤活性方面,甲氧基化合物4e和6e对三种肿瘤细胞系均表现出显著的细胞毒活性。化合物4e、5e和6e显示出较强的铁离子(Fe3+)还原抗氧化能力(FRAP)。化合物5b在各浓度下对Fe2+离子的螯合活性均较强。
Synthesis of Schiff Base Indolyl-1,3,4-Oxadiazole, Thiazolidinone and Azetidinone as Efficient Antimicrobial, Antioxidant, Antituberculosis and Anticancer Agents
The present investigation was under-taken to synthesize the Schiff base indole derivatives bearing of 1,3,4-oxadiazole thiazolidinone and azetidinone moieties. New series of 5-(5-substituted-3-phenyl-1H-indol-2-yl)-N-[(5-substituted-2-phenyl-1H-indol-3-yl)methylene]-1,3,4-oxadiazol-2-amines and screened their biological activities. Compound 4a showed excellent antibacterial and radical scavenging activities. Compound 5a revealed efficient to antifungal activity. In addition, compound 4a was found to be most active against H37Rv strain Mycobacterium tuberculosis. In case of anticancer activity methoxy compounds 4e and 6e against all the three tumor cell lines manifested remarkable cytotoxic activity. Compounds 4e, 5e and 6e have shown strong ferrous ions (Fe3+) reducing antioxidant power (FRAP) among the compounds screened. Compound 5b showed more potent of metal chelating on Fe2+ ions activity at all concentrations.