文章基本信息

标题：Synthesis of novel indole, 1,2,4-triazole derivatives as potential glucosidase inhibitors
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作者：Ramesh S Gani ; Karabasanagouda Timanagouda ; S. Madhushree 等
期刊名称：Journal of King Saud University - Science
印刷版ISSN：1018-3647
出版年度：2020
卷号：32
期号：8
页码：3388-3399
DOI：10.1016/j.jksus.2020.09.026
语种：English
出版社：Elsevier
摘要：Graphical abstractDisplay OmittedAbstractObjectiveIn the present study a series of eleven bis-heterocyclic compounds with indole derivative carrying 1,2,4-triazole moiety were synthesized and assessed for theirin vitroα-amylase and α-glucosidase inhibition activity.MethodThe synthesized compounds were characterized by using various spectroscopic techniques such as1H NMR, IR and EI-MS. Initialin silicoscreening process was used to find potential ligands that were later evaluated for α-amylase and α-glucosidase inhibitory potential.ResultsThe docking results revealed that the synthesized compounds were well accommodated in the binding pockets of α-glucosidase. Especially,5eand5jshowed similar interaction pattern, as previously reported Casuarine-enzyme complex.In vitroanalysis suggests that compounds5a-5kshowed varying degrees of α-amylase and α-glucosidase inhibitory activity. Amongst them,5eand5jdemonstrated good enzyme inhibition while remaining compounds showed low to moderate inhibitory potential.ConclusionsAddition of 2,5 dimethoxy substituent (2,5-dimethoxybenzaldehyde) (5e)or hydroxy, methoxy substituents (6-methoxy-2-naphthol aldehyde) (5j)at ortho and meta position exhibited good α-amylase and α-glucosidase inhibition. Hence this study provides several insights on improving the pharmacological profile of triazole containing compounds that can be adopted to design and develop novel glucosidase inhibitors.
关键词：α-Amylase;α-Glucosidase;Molecular docking;Indole;Triazole