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Ugi Four-Multicomponent Reaction Based Synthesis, in Vitro, and in Silico Enzymatic Evaluations of New Pyrazino[1,2-A]Indole-1,4-Dione-Indole-2-Phenylacetamides As Potent Inhibitors Against Α-Glucosidase and Α-Amylase Publisher Pubmed



Ahmadi Shourkaei F1 ; Rashidi Ranjbar P1 ; Taslimi P2 ; Mahdavi M3
Authors
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Authors Affiliations
  1. 1. School of Chemistry, College of Science, University of Tehran, Tehran, Iran
  2. 2. Department of Biotechnology, Faculty of Science, Bartin University, Bartin, Turkey
  3. 3. Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran

Source: Chemistry and Biodiversity Published:2024


Abstract

In this work, synthesis and evaluation of pyrazino[1,2-a]indole-1,4-dione-indole-2-phenylacetamides 6 a–k as new synthetic anti-diabetes agents were presented. These compounds were synthesized by a four-component Ugi reaction without metal catalyst. All synthesized compounds were evaluated against α-glucosidase and α-amylase as two important targets in the treatment of diabetes. Approximately, all new compounds 6 a–k were more potent than positive control acarbose against these studied enzymes. The obtained potent compounds against the target enzymes were docked in the active site of the related enzyme. Docking study showed that our new potent compounds as well interacted with key residues of the target enzyme. © 2023 Wiley-VHCA AG, Zurich, Switzerland.