Tehran University of Medical Sciences

Science Communicator Platform

Stay connected! Follow us on X network (Twitter):
Share this content! By
New Phthalimide-Benzamide-1,2,3-Triazole Hybrids; Design, Synthesis, Α-Glucosidase Inhibition Assay, and Docking Study Publisher



Sadatebrahimi SE1 ; Rahmani A1 ; Mohammadikhanaposhtani M2 ; Jafari N3 ; Mojtabavi S4 ; Ali Faramarzi M4 ; Emadi M5 ; Yahyameymandi A6 ; Larijani B7 ; Biglar M7 ; Mahdavi M7
Authors

Source: Medicinal Chemistry Research Published:2020


Abstract

A new series of phthalimide-benzamide-1,2,3-triazole hybrids 8a–k as α-glucosidase inhibitors was designed and synthesized. The biological evaluation of compounds 8a–k against yeast α-glucosidase demonstrated that all they have excellent inhibitory activity in comparison with standard inhibitor acarbose. Among them, the most potent compound was compound 8d with inhibitory activity 18.5-fold more than acarbose. Kinetic study revealed that α-glucosidase inhibition of compound 8d was the competitive type. Furthermore, docking study suggested that compound 8d is more stable than acarbose in the active site of α-glucosidase. © 2020, Springer Science+Business Media, LLC, part of Springer Nature.
Related Docs
View other Related Docs
1. Synthesis and Biological Evaluation of New Benzimidazole-1,2,3-Triazole Hybrids As Potential Α-Glucosidase Inhibitors, Bioorganic Chemistry (2020)
2. 2,4-Dioxochroman Moiety Linked to 1,2,3-Triazole Derivatives As Novel Α-Glucosidase Inhibitors: Synthesis, in Vitro Biological Evaluation, and Docking Study, Current Organic Chemistry (2020)
3. New Acridine-9-Carboxamide Linked to 1,2,3-Triazole-N-Phenylacetamide Derivatives As Potent Α-Glucosidase Inhibitors: Design, Synthesis, in Vitro, and in Silico Biological Evaluations, Medicinal Chemistry Research (2020)
Experts (# of related papers)
View all Related Experts
Mohammad Ali Faramarzi (19)
Mohammad Mahdavi (18)
Other Related Docs
4. A Review on Synthesis, Mechanism of Action, and Structure-Activity Relationships of 1,2,3-Triazole-Based Α-Glucosidase Inhibitors As Promising Anti-Diabetic Agents, Journal of Molecular Structure (2022)
5. Design and Synthesis of Novel Quinazolinone-Pyrazole Derivatives As Potential Α-Glucosidase Inhibitors: Structure-Activity Relationship, Molecular Modeling and Kinetic Study, Bioorganic Chemistry (2021)
6. New Thiosemicarbazide-1,2,3-Triazole Hybrids As Potent Α-Glucosidase Inhibitors: Design, Synthesis, and Biological Evaluation, Journal of Molecular Structure (2019)
7. Design, Synthesis, in Vitro, and in Silico Studies of Novel Diarylimidazole-1,2,3-Triazole Hybrids As Potent Α-Glucosidase Inhibitors, Bioorganic and Medicinal Chemistry (2019)
8. Design and Synthesis of Phenoxymethybenzoimidazole Incorporating Different Aryl Thiazole-Triazole Acetamide Derivatives As Α-Glycosidase Inhibitors, Molecular Diversity (2022)
9. 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)
10. Biscoumarin-1,2,3-Triazole Hybrids As Novel Anti-Diabetic Agents: Design, Synthesis, in Vitro Α-Glucosidase Inhibition, Kinetic, and Docking Studies, Bioorganic Chemistry (2019)
11. An Efficient and Targeted Synthetic Approach Towards New Highly Substituted 6-Amino-Pyrazolo[1,5-A]Pyrimidines With Α-Glucosidase Inhibitory Activity, Scientific Reports (2020)
12. In Silico and in Vitro Studies of Thiosemicarbazone-Indole Hybrid Compounds As Potent Α-Glycosidase Inhibitors, Computational Biology and Chemistry (2022)
13. Design, Synthesis Docking and Molecular Dynamics Studies of 2-Amino-4-Phenylthiazole-Indole Hybrids As Α-Glucosidase Inhibitors, Journal of Molecular Structure (2024)
14. Synthesis and Structure–Activity Relationship Studies of Benzimidazole-Thioquinoline Derivatives As Α-Glucosidase Inhibitors, Scientific Reports (2023)
15. Design, Synthesis, Molecular Docking, and in Vitro Α-Glucosidase Inhibitory Activities of Novel 3-Amino-2,4-Diarylbenzo[4,5]Imidazo[1,2-A]Pyrimidines Against Yeast and Rat Α-Glucosidase, Scientific Reports (2021)
16. Synthesis, in Vitro Evaluation, and Molecular Docking Studies of Novel Hydrazineylideneindolinone Linked to Phenoxymethyl-1,2,3-Triazole Derivatives As Potential Α-Glucosidase Inhibitors, Bioorganic Chemistry (2021)
17. Design of New Α-Glucosidase Inhibitors Based on the Bis-4-Hydroxycoumarin Skeleton: Synthesis, Evaluation, and in Silico Studies, Scientific Reports (2024)
18. Synthesis of the New Tri-Amide Derivatives As Novel Α-Glucosidase Inhibitors by Ugi Four-Component Reaction, Journal of Molecular Structure (2021)
19. Design and Synthesis of Novel 5-Arylisoxazole-1,3,4-Thiadiazole Hybrids As Α-Glucosidase Inhibitors, Letters in Drug Design and Discovery (2021)
20. Synthesis, in Vitro, and in Silico Evaluation of Indazole Schiff Bases As Potential Α-Glucosidase Inhibitors, Journal of Molecular Structure (2021)