Mechanochemical Synthesis of Thiazolidinone-Triazoles Derivatives as Antidiabetic Agents: Pharmacokinetics, Molecular Docking, and In Vitro Antidiabetic Properties

M B Taj; A Raheel; W Alelwani; A M Alnajeebi; R B Alnoman; T Javed

doi:10.1134/S1070363223040199

Mechanochemical Synthesis of Thiazolidinone-Triazoles Derivatives as Antidiabetic Agents: Pharmacokinetics, Molecular Docking, and In Vitro Antidiabetic Properties

Russ J Gen Chem. 2023;93(4):912-919. doi: 10.1134/S1070363223040199. Epub 2023 May 25.

Authors

M B Taj¹, A Raheel², W Alelwani³, A M Alnajeebi³, R B Alnoman⁴, T Javed⁵

Affiliations

¹ Institute of Chemistry, Islamia University Bahawalpur, 63100 Bahawalpur, Pakistan.
² Department of Chemistry, Quaid-e-Azam University, 44000 Islamabad, Pakistan.
³ Department of Biochemistry, College of Science, University of Jeddah, Jeddah, Saudi Arabia.
⁴ Faculty of Science, Chemistry Department, Taibah University, Yanbu Branch, Yanbu, Saudi Arabia.
⁵ Department of Chemistry, University of Sahiwal, 57000 Sahiwal, Pakistan.

Abstract

Mechanochemistry is an eco-friendly and solventless method. In the present study, the surface of a custom-made closed mortar and pestle is used as a catalyst to synthesize thiazolidinone-triazole derivatives successfully. The compounds were subjected to potential antidiabetic activity. The results showed that para-chloro-substituted derivative (9c) is most active with IC₅₀ values of 10±1.56. All three compounds 9a-9c with a maximum of 20% inhibition for ALR1 represent superior selectivity toward the targeted ALR2 to act as a lead in the search for new antidiabetic agents.

Keywords: CuAAC reaction; antidiabetic potential; molecular docking; surface scratching; thiazole derivatives.