Tehran University of Medical Sciences

Science Communicator Platform

Stay connected! Follow us on X network (Twitter):
Share By
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

Summary: Can new molecules fight diabetes? Research shows pyrazino-indole compounds strongly inhibit diabetes enzymes, promising better treatment options. #DiabetesCare #DrugSynthesis

Ahmadi Shourkaei F1 ; Rashidi Ranjbar P1 ; Taslimi P2 ; Mahdavi M3
Authors

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.
Related Docs
View other Related Docs
1. Synthesis and Biological Evaluation of New Dihydroindolizino[8,7-B]Indole Derivatives As Novel Α-Glucosidase Inhibitors, Journal of Molecular Structure (2021)
2. Ugi Adducts: Design and Synthesis of Natural-Based Α-Glucosidase Inhibitors, Letters in Organic Chemistry (2022)
3. Cyanoacetohydrazide Linked to 1,2,3-Triazole Derivatives: A New Class of Α-Glucosidase Inhibitors, Scientific Reports (2022)
Experts (# of related papers)
View all Related Experts
Mohammad Ali Faramarzi (17)
Mohammad Mahdavi (14)
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
Other Related Docs
4. Synthesis and Bioactivities Evaluation of Quinazolin-4(3H)-One Derivatives As Α-Glucosidase Inhibitors, BMC Chemistry (2022)
5. Development of Coumarin Tagged 1,2,3-Triazole Derivatives Targeting Α-Glucosidase Inhibition: Synthetic Modification, Biological Evaluation, Kinetic and in Silico Studies, Journal of Molecular Structure (2023)
6. Design, Synthesis, in Vitro Anti-Α-Glucosidase Evaluations, and Computational Studies of New Phthalimide-Phenoxy-1,2,3-Triazole-N-Phenyl (Or Benzyl) Acetamides As Potential Anti-Diabetic Agents, Scientific Reports (2023)
7. Evaluation of Novel 2-(Quinoline-2-Ylthio)Acetamide Derivatives Linked to Diphenyl-Imidazole As Α-Glucosidase Inhibitors: Insights From in Silico, in Vitro, and in Vivo Studies on Their Anti-Diabetic Properties, European Journal of Medicinal Chemistry (2024)
8. Quinoline-Piperazine Derivatives As Potential Α-Glucosidase Inhibitors: Synthesis, Biological Evaluation, and in Silico Studies, Journal of Molecular Structure (2025)
9. Study on the Interaction of 1,5-Diaryl Pyrrole Derivatives With Αglucosidase; Synthesis, Molecular Docking, and Kinetic Study, Medicinal Chemistry (2021)
10. Experimental and Computational Evidence for Kot-Bu-Promoted Synthesis of Oxopyrazino[1,2-A]Indoles, RSC Advances (2015)
11. Synthesis and Biological Assessment of Benzimidazole-Acrylonitrile-1,2,3-Triazole Derivatives As Α-Glucosidase Inhibitors, Bioorganic Chemistry (2025)
12. Design and Synthesis of New Imidazo[1,2-B]Pyrazole Derivatives, in Vitro Α-Glucosidase Inhibition, Kinetic and Docking Studies, Molecular Diversity (2020)
13. Design, Synthesis, and Evaluation of Triazolo[1,5-A]Pyridines As Novel and Potent Α‑Glucosidase Inhibitors, Scientific Reports (2025)
14. Design and Synthesis of Novel Pyrazole-Phenyl Semicarbazone Derivatives As Potential Α-Glucosidase Inhibitor: Kinetics and Molecular Dynamics Simulation Study, International Journal of Biological Macromolecules (2021)
15. Docking Study, Molecular Dynamic, Synthesis, Anti-Α-Glucosidase Assessment, and Admet Prediction of New Benzimidazole-Schiff Base Derivatives, Scientific Reports (2022)
16. Design, Synthesis, in Vitro, and in Silico Evaluations of Benzo[D]Imidazole-Amide-1,2,3-Triazole-N-Arylacetamide Hybrids As New Antidiabetic Agents Targeting Α-Glucosidase, Scientific Reports (2023)
17. Preparation of Novel 3,4,5-Triaryl-1,2,4-Oxadiazole Derivatives: Molecular Docking and Α-Glucosidase Assessment, ChemistrySelect (2024)
18. Synthesis, Biological Activities, and Molecular Docking Studies of Triazolo[4,3-B]Triazine Derivatives As a Novel Class of Α-Glucosidase and Α-Amylase Inhibitors, Archiv der Pharmazie (2024)
19. In Silico and in Vitro Studies of Thiosemicarbazone-Indole Hybrid Compounds As Potent Α-Glycosidase Inhibitors, Computational Biology and Chemistry (2022)
20. Design, Synthesis Docking and Molecular Dynamics Studies of 2-Amino-4-Phenylthiazole-Indole Hybrids As Α-Glucosidase Inhibitors, Journal of Molecular Structure (2024)