Tehran University of Medical Sciences

Science Communicator Platform

Stay connected! Follow us on X network (Twitter):
Share this content! By
Α-Glucosidase Inhibition Assay of Galbanic Acid and It Amide Derivatives: New Excellent Semi-Synthetic Α-Glucosidase Inhibitors Publisher Pubmed



Mohammadikhanaposhtani M1 ; Sayahi MH2, 3 ; Yazzaf R4 ; Dastyafteh N4 ; Halimi M5 ; Iraji A6, 7, 8 ; Dadgar A4 ; Mojtabavi S9 ; Faramarzi MA9 ; Palimi M10 ; Mirzazadeh R11 ; Larijani B4 ; Delnavazi MR12 ; Mahdavi M4, 13
Authors

Source: Bioorganic Chemistry Published:2024


Abstract

α-Glucosidase inhibitory activity of galbanic acid and its new amide derivatives 3a–n were investigated. Galbanic acid and compounds 3a–n showed excellent anti-α-glucosidase activity with IC50 values ranging from 0.3 ± 0.3 μM to 416.0 ± 0.2 μM in comparison to positive control acarbose with IC50 value of = 750.0 ± 5.6. In the kinetic study, the most potent compound 3h demonstrated a competitive mode of inhibition with Ki = 0.57 µM. The interaction of the most potent compound 3h with the α-glucosidase was further elaborated by in vitro Circular dichroism assessment and in silico molecular docking and Molecular dynamics studies. Compound 3h was also non-cytotoxic on human normal cells. In silico study on pharmacokinetics and toxicity profile of the most potent galbanic acid derivatives demonstrated that these compounds are valuable lead compounds for further study in order to achieve new anti-diabetic agents. © 2024 Elsevier Inc.
Related Docs
View other Related Docs
1. Coumarin-Based Scaffold As Α-Glucosidase Inhibitory Activity: Implication for the Development of Potent Antidiabetic Agents, Mini-Reviews in Medicinal Chemistry (2020)
2. Design, Synthesis, in Vitro, and in Silico Biological Evaluations of Coumarin-Indole Hybrids As New Anti-Α-Glucosidase Agents, BMC Chemistry (2022)
3. Design and Synthesis of Novel Quinazolinone-Pyrazole Derivatives As Potential Α-Glucosidase Inhibitors: Structure-Activity Relationship, Molecular Modeling and Kinetic Study, Bioorganic Chemistry (2021)
Experts (# of related papers)
View all Related Experts
Mohammad Ali Faramarzi (19)
Mohammad Mahdavi (16)
Other Related Docs
4. Synthesis and Structure–Activity Relationship Studies of Benzimidazole-Thioquinoline Derivatives As Α-Glucosidase Inhibitors, Scientific Reports (2023)
5. A New Route to the Synthesis of 2-Hydrazolyl-4-Thiazolidinone Hybrids, Evaluation of Α-Glucosidase Inhibitory Activity and Molecular Modeling Insights, Heliyon (2024)
6. 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)
7. 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)
8. In Silico and in Vitro Studies of Thiosemicarbazone-Indole Hybrid Compounds As Potent Α-Glycosidase Inhibitors, Computational Biology and Chemistry (2022)
9. Design, Synthesis Docking and Molecular Dynamics Studies of 2-Amino-4-Phenylthiazole-Indole Hybrids As Α-Glucosidase Inhibitors, Journal of Molecular Structure (2024)
10. Design, Synthesis, in Vitro, and in Silico Enzymatic Evaluations of Thieno[2,3-B]Quinoline-Hydrazones As Novel Inhibitors for Α-Glucosidase, Bioorganic Chemistry (2022)
11. Imidazo[1,2-C]Quinazolines As a Novel and Potent Scaffold of Α-Glucosidase Inhibitors: Design, Synthesis, Biological Evaluations, and in Silico Studies, Scientific Reports (2023)
12. New Thiosemicarbazide-1,2,3-Triazole Hybrids As Potent Α-Glucosidase Inhibitors: Design, Synthesis, and Biological Evaluation, Journal of Molecular Structure (2019)
13. Design, Synthesis, Docking Study, Α-Glucosidase Inhibition, and Cytotoxic Activities of Acridine Linked to Thioacetamides As Novel Agents in Treatment of Type 2 Diabetes, Bioorganic Chemistry (2018)
14. Design of New Α-Glucosidase Inhibitors Based on the Bis-4-Hydroxycoumarin Skeleton: Synthesis, Evaluation, and in Silico Studies, Scientific Reports (2024)
15. Synthesis and Biological Evaluation of New Dihydroindolizino[8,7-B]Indole Derivatives As Novel Α-Glucosidase Inhibitors, Journal of Molecular Structure (2021)
16. Pyrano[3,2-C]Quinoline Derivatives As New Class of Α-Glucosidase Inhibitors to Treat Type 2 Diabetes: Synthesis, in Vitro Biological Evaluation and Kinetic Study, Medicinal Chemistry (2019)
17. Novel N′-Substituted Benzylidene Benzohydrazides Linked to 1,2,3-Triazoles: Potent Α-Glucosidase Inhibitors, Scientific Reports (2023)
18. New Phenylthiosemicarbazide-Phenoxy-1,2,3-Triazole-N-Phenylacetamides As Dual Inhibitors Against Α-Glucosidase and Ptp-1B for the Treatment of Type 2 Diabetes, Archiv der Pharmazie (2024)
19. Design, Synthesis, and Molecular Docking Studies of Diphenylquinoxaline-6-Carbohydrazide Hybrids As Potent Α-Glucosidase Inhibitors, BMC Chemistry (2022)
20. 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)