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

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 Publisher

Seyfi S¹ ; Salarinejad S² ; Moghimi S¹ ; Toolabi M³ ; Sadeghian N⁴ ; Tuzun B⁵ ; Firoozpour L^{1, 2} ; Ketabforoosh SHME⁶ ; Taslimi P⁴ ; Foroumadi A^{1, 2}

Show Affiliations

1. Drug Design and Development Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, Iran
2. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
3. Department of Medicinal Chemistry, School of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran
4. Department of Biotechnology, Faculty of Science, Bartin University, Bartin, Turkey
5. Plant and Animal Production Department, Technical Sciences Vocational School of Sivas, Sivas Cumhuriyet University, Sivas, Turkey
6. Department of Medicinal Chemistry, School of Pharmacy, Alborz University of Medical Science, Karaj, Iran

Source: Archiv der Pharmazie Published:2024

Abstract

In diabetes mellitus, amylase and glucosidase enzymes are the primary triggers. The main function of these enzymes is to break macromolecules into simple sugar units, which directly affect blood sugar levels by increasing blood permeability. To overcome this metabolic effect, there is a need for a potent and effective inhibitor capable of suppressing the enzymatic conversion of sugar macromolecules into their smaller units. Herein, we reported the discovery of a series of substituted triazolo[4,3-b][1,2,4]triazine derivatives as α-glucosidase and α-amylase inhibitors. All target compounds demonstrated significant inhibitory activities against α-glucosidase and α-amylase enzymes compared with acarbose as the positive control. The most potent compound 10k, 2-[(6-phenyl-[1,2,4]triazolo[4,3-b][1,2,4]triazin-3-yl)thio]-N-[4-(trifluoromethyl)phenyl]acetamide, demonstrated IC50 values of 31.87 and 24.64 nM against α-glucosidase and α-amylase enzymes, respectively. To study their mechanism of action, kinetic studies were also done, which determined the mode of inhibition of both enzymes. Molecular docking was used to confirm the binding interactions of the most active compounds. © 2024 Deutsche Pharmazeutische Gesellschaft.

Style	Citing Format
MLA	Seyfi S, et al.. "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, vol. , no. , 2024, pp. -.
APA	Seyfi S, Salarinejad S, Moghimi S, Toolabi M, Sadeghian N, Tuzun B, Firoozpour L, Ketabforoosh SHME, Taslimi P, Foroumadi A (2024). 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, (), -.
Chicago	Seyfi S, Salarinejad S, Moghimi S, Toolabi M, Sadeghian N, Tuzun B, Firoozpour L, Ketabforoosh SHME, Taslimi P, Foroumadi A. "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 , no. (2024): -.
Harvard	Seyfi S et al. (2024) '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, (), pp. -.
Vancouver	Seyfi S, Salarinejad S, Moghimi S, Toolabi M, Sadeghian N, Tuzun B, et al.. 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;():-.
BibTex	@article{ author = {Seyfi S and Salarinejad S and Moghimi S and Toolabi M and Sadeghian N and Tuzun B and Firoozpour L and Ketabforoosh SHME and Taslimi P and Foroumadi A}, title = {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}, journal = {Archiv der Pharmazie}, volume = {}, number = {}, pages = {-}, year = {2024} }
RIS	TY - JOUR AU - Seyfi S AU - Salarinejad S AU - Moghimi S AU - Toolabi M AU - Sadeghian N AU - Tuzun B AU - Firoozpour L AU - Ketabforoosh SHME AU - Taslimi P AU - Foroumadi A TI - 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 JO - Archiv der Pharmazie VL - IS - SP - EP - PY - 2024 ER -

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