Synthesis, α-Glucosidase Inhibitory Activity and Molecular Docking Study of Chalcone Derivatives Bearing a 1H-1,2,3-Triazole Unit

Bayu Ardiansah, Nur Rohman, Mochammad Arfin Fardiansyah Nasution, Hiroki Tanimoto, Antonius Herry Cahyana, Arif Fadlan, Titin Ariyani

Research output: Contribution to journalArticlepeer-review

3 Citations (Scopus)

Abstract

Diabetes mellitus (DM) is a metabolic condition that is a major health concern around the world. The current study investigates the synthesis of a series of chalcone and 1H-1,2,3-triazole hybrid compounds and their in vitro inhibitory potential against α-glucosidase. The antidiabetic analysis revealed that compounds 4a and 4b are highly active agents with IC50 of 3.90 and 4.77 µM, respectively. These results are close to quercetin (IC50 = 4.24 µM) as the reference standard. Molecular docking study strongly supports the active interaction of the 4a and 4b to the enzyme through cation-π interaction and hydrogen bonding between the ligands and the active site of Saccharomyces cerevisiae α-glucosidase enzyme. This study broadened the potential of designing chalcone-triazole hybrid compounds as antidiabetic drug candidates in the pharmaceutical sector.

Original languageEnglish
Pages (from-to)342-348
Number of pages7
JournalChemical & pharmaceutical bulletin
Volume71
Issue number5
DOIs
Publication statusPublished - 2023

Keywords

  • 1H-1,2,3-triazole
  • antidiabetic
  • chalcone
  • hybrid compound
  • Saccharomyces cerevisiae α-glucosidase

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