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

Author:

Shafique Kainat1,Farrukh Aftab2,Mahmood Ali Tariq3,Qasim Sumera4,Jafri Laila5,Abd-Rabboh Hisham S. M.6,AL-Anazy Murefah mana7,Kalsoom Saima8

Affiliation:

1. SA-Center for Interdisciplinary Research in Basic Sciences, International Islamic University, Islamabad 44000, Pakistan

2. Department of Physics, PMAS-Arid Agriculture University, Rawalpindi 44000, Pakistan

3. Health Services Academy, Islamabad 44000, Pakistan

4. Department of Pharmacology, College of Pharmacy, Jouf University, Sakaka 72431, Saudi Arabia

5. Department of Life Sciences, Abasyn University, Islamabad Campus, Islamabad 44000, Pakistan

6. Chemistry Department, Faculty of Science, King Khalid University, P.O. Box 9004, Abha 61413, Saudi Arabia

7. Department of Chemistry, College of Sciences, Princess Nourah bint Abdulrahman University (PNU), P.O. Box 84428, Riyadh 11671, Saudi Arabia

8. Department of Chemistry, PMAS-Arid Agriculture University, Rawalpindi 44000, Pakistan

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.

Publisher

MDPI AG

Subject

Chemistry (miscellaneous),Analytical Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Molecular Medicine,Drug Discovery,Pharmaceutical Science

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