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Synthesis, Α-Glucosidase Inhibitory Activity and Docking Studies of Novel Ethyl 1,2,3-Triazol-4-Ylmethylthio-5,6-Diphenylpyridazine-4-Carboxylate Derivatives Publisher



Firoozpour L1 ; Moghimi S2 ; Salarinejad S1 ; Toolabi M3 ; Rafsanjani M1 ; Pakrad R4 ; Salmani F4 ; Shokrolahi SM4 ; Sadat Ebrahimi SE1 ; Karima S4 ; Foroumadi A1, 2
Authors
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Authors Affiliations
  1. 1. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  2. 2. Drug Design and Development Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, Iran
  3. 3. Department of Medicinal Chemistry, School of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran
  4. 4. Department of Clinical Biochemistry, School of Medicine, Shahid Beheshti University of Medical Sciences (SBMU), Tehran, Iran

Source: BMC Chemistry Published:2023


Abstract

In this work, a novel series of pyridazine-triazole hybrid molecules were prepared and evaluated as inhibitors of rat intestinal α-glucosidase enzyme. Amongst all newly synthesized compounds, 10k showed good inhibition in the series with IC50 value of 1.7 µM which is 100 folds stronger than positive control, acarbose. The cytotoxicity revealed that this compound is not toxic against normal cell line, HDF. The docking studies showed that triazole ring plays an important role in the binding interactions with the active site. The insertion of compound 10k into the active pocket of α-glucosidase and formation of hydrogen bonds with Leu677 was observed from docking studies. The kinetic studies revealed that this compound has uncompetitive mode of inhibition against α-glucosidase enzyme. © 2023, The Author(s).
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