Synthesis, Characterization and in vitro Studies of Some Ethyl 2-Carboxylate-5- monosubstitued 1H-indole Derivatives as Potential GSK-3β Inhibitors

D. Ramesh, Chatpalliwar Vivekanand Arvind
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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.
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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
由于吲哚衍生物对GSK-3β具有良好的抑制活性,因此目前的研究重点是吲哚衍生物。采用Japp-Klingemann吲哚合成法合成了基于吲哚部分的新化合物。通过FTIR、1H NMR、13C NMR、GC-HRMS和元素分析对新化合物的结构进行了鉴定。采用IC50光度法评价新化合物体外GSK-3β抑制活性。化合物Aii11表现出良好的抑制活性。化合物Aii2、Aii1和Aii3具有良好的GSK-3β抑制活性。
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