Please use this identifier to cite or link to this item: http://ir.lib.seu.ac.lk/handle/123456789/5819
Title: Synthesis of 1,2,3,triazole modified analogues of hydrochlorothiazide via click chemistry approach and in‑vitro α‑glucosidase enzyme inhibition studies
Authors: Hina, Siddiqui
Baheej, M. A. A.
Saeed Ullah
Fazila, Rizvi
Shazia, Iqbal
Haroon, M. H.
Atia‑tul Wahab
Iqbal Choudhary, M.
Keywords: Click Chemistry
Diabetes
A-Glucosidase Enzyme
Hydrochlorothiazide
1,2,3-Triazole Derivatives
Cytotoxicity
Issue Date: 4-Oct-2021
Publisher: Springer Nature Switzerland AG 202
Citation: Molecular Diversity, 2021
Abstract: The current study was aimed to discover potent inhibitors of the α-glucosidase enzyme. A 25 membered library of new 1,2,3-triazole derivatives of hydrochlorothiazide (1) (HCTZ, a diuretic drug also being used for the treatment of high blood pressure) was synthesized through the click chemistry approach. The structures of all derivatives 2–26 were deduced by MS, IR, 1 H NMR, and 13C-NMR spectroscopic techniques. All the compounds were found to be new. Compounds 1–26 were evaluated for α-glucosidase enzyme inhibition activity. Among them, 18 compounds showed potent inhibitory activity against α-glucosidase with IC50 values between 24 and 379 µM. α-Glucosidase inhibitor drug acarbose (IC50=875.75±2.08 μM) was used as the standard. Kinetics studies of compounds 6, 9, 11, 12, 15, 20, 23, and 24 revealed that only compound 15 was a mixed-type of inhibitor, while others were non-competitive inhibitors of the α-glucosidase enzyme. All the compounds were found to be non-cytotoxic when checked against the mouse fibroblast 3T3 cell line.
URI: https://doi.org/10.1007/s11030-021-10314-3
http://ir.lib.seu.ac.lk/handle/123456789/5819
ISSN: 1573-501X
Appears in Collections:Research Articles

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