{"title":"2-羧酸乙酯-5-单取代1h -吲哚衍生物的合成、表征及体外研究","authors":"D. Ramesh, Chatpalliwar Vivekanand Arvind","doi":"10.14233/ajomc.2022.ajomc-p390","DOIUrl":null,"url":null,"abstract":"The present work focuses on indole derivatives due to their promising inhibition activity toward GSK-3β. New compounds based on the indole moiety were synthesized via Japp-Klingemann indole synthesis. The structures of the new compounds were elucidated on the basis of their FTIR, 1H NMR, 13C NMR spectral data, GC-HRMS and elemental analysis. The in vitro GSK-3β inhibitory activity of the new compounds was evaluated using a luminance assay technique in terms of IC50. Compound Aii11 showed excellent inhibitory activity. Compounds Aii2, Aii1 and Aii3 presented promising GSK-3β inhibitory activity.","PeriodicalId":8544,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"43 1","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis, Characterization and in vitro Studies of Some Ethyl 2-Carboxylate-5-\\nmonosubstitued 1H-indole Derivatives as Potential GSK-3β Inhibitors\",\"authors\":\"D. Ramesh, Chatpalliwar Vivekanand Arvind\",\"doi\":\"10.14233/ajomc.2022.ajomc-p390\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"The present work focuses on indole derivatives due to their promising inhibition activity toward GSK-3β. New compounds based on the indole moiety were synthesized via Japp-Klingemann indole synthesis. The structures of the new compounds were elucidated on the basis of their FTIR, 1H NMR, 13C NMR spectral data, GC-HRMS and elemental analysis. The in vitro GSK-3β inhibitory activity of the new compounds was evaluated using a luminance assay technique in terms of IC50. Compound Aii11 showed excellent inhibitory activity. Compounds Aii2, Aii1 and Aii3 presented promising GSK-3β inhibitory activity.\",\"PeriodicalId\":8544,\"journal\":{\"name\":\"Asian Journal of Organic & Medicinal Chemistry\",\"volume\":\"43 1\",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2022-01-01\",\"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.2022.ajomc-p390\",\"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.2022.ajomc-p390","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Synthesis, Characterization and in vitro Studies of Some Ethyl 2-Carboxylate-5-
monosubstitued 1H-indole Derivatives as Potential GSK-3β Inhibitors
The present work focuses on indole derivatives due to their promising inhibition activity toward GSK-3β. New compounds based on the indole moiety were synthesized via Japp-Klingemann indole synthesis. The structures of the new compounds were elucidated on the basis of their FTIR, 1H NMR, 13C NMR spectral data, GC-HRMS and elemental analysis. The in vitro GSK-3β inhibitory activity of the new compounds was evaluated using a luminance assay technique in terms of IC50. Compound Aii11 showed excellent inhibitory activity. Compounds Aii2, Aii1 and Aii3 presented promising GSK-3β inhibitory activity.