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Synthesis, In-Vitro Evaluation, Molecular Docking, and Kinetic Studies of Pyridazine-Triazole Hybrid System As Novel Α-Glucosidase Inhibitors Publisher Pubmed



Moghimi S1 ; Salarinejad S2 ; Toolabi M3 ; Firoozpour L1 ; Esmaeil Sadat Ebrahimi S2 ; Safari F4 ; Madaniqamsari F1 ; Mojtabavi S5 ; Faramarzi MA5 ; Karima S6 ; Pakrad R6 ; Foroumadi A1, 2
Authors

Source: Bioorganic Chemistry Published:2021


Abstract

In this study, we reported the discovery of pyridazine based 1,2,3-triazole derivatives as inhibitors of α-glucosidase. All target compounds exhibited significant inhibitory activities against yeast and rat α-glucosidase enzymes compared to positive control, acarbose. The most potent compound 6j, ethyl 3-(2-(1-(4-nitrobenzyl)-1H-1,2,3-triazol-4-yl)ethyl)-5,6-diphenylpyridazine-4-carboxylate exhibited IC50 values of 58, and 73 µM. Docking studies indicated the responsibility of hydrophobic and hydrogen bonding interactions in the ligand-enzyme complex stability. The in-vitro safety against the normal cell line was observed by toxicity evaluation of the selected compounds. © 2021 Elsevier Inc.
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