Designing Click One-Pot Synthesis and Antidiabetic Studies of 1,2,3-Triazole Derivatives

Molecules. 2023 Mar 30;28(7):3104. doi: 10.3390/molecules28073104.

Abstract

In the present study, a new series of 1,2,3-triazole derivatives was synthesized via a click one-pot reaction. The synthesized compounds were found to be active during molecular docking studies against targeted protein 1T69 by using the Molecular Operating Environment (MOE) software. The designed and synthesized compounds were characterized by using FT-IR, 1H-NMR and LC-MS spectra. The synthesized triazole moieties were further screened for their α-amylase and α-glucosidase inhibitory activities. The preliminary activity analysis revealed that all the compounds showed good inhibition activity, ranging from moderate to high depending upon their structures and concentrations and compared to the standard drug acarbose. Both in silico and in vitro analysis indicated that the synthesized triazole molecules are potent for DM type-II. Out of all the compounds, compound K-1 showed the maximum antidiabetic activity with 87.01% and 99.17% inhibition at 800 µg/mL in the α-amylase and α-glucosidase inhibition assays, respectively. Therefore these triazoles may be further used as promising molecules for development of antidiabetic compounds.

Keywords: antidiabetic assay molecular docking; diabetes mellitus; triazole derivatives.

MeSH terms

  • Glycoside Hydrolase Inhibitors / chemistry
  • Hypoglycemic Agents* / chemistry
  • Molecular Docking Simulation
  • Molecular Structure
  • Spectroscopy, Fourier Transform Infrared
  • Structure-Activity Relationship
  • Triazoles / chemistry
  • Triazoles / pharmacology
  • alpha-Amylases / metabolism
  • alpha-Glucosidases* / metabolism

Substances

  • Hypoglycemic Agents
  • alpha-Glucosidases
  • Glycoside Hydrolase Inhibitors
  • Triazoles
  • alpha-Amylases

Grants and funding

We are also highly grateful for the support of Sumera Qasim, Jouf University, Saudi Arabia. This research was also supported by Princess Nourah bint Abdulrahman University Researchers Supporting Project number (PNURSP2023R7), Princess Nourah bint Abdulrahman University, Riyadh, Saudi Arabia. The authors extend their appreciation to the Deanship of Scientific Research at King Khalid University for funding this work through the Large Groups Project under grant number (RGP.2/228/44).