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Synthesis and Characterization of 1-Amidino-O-Alkylureas Metal Complexes As Α- Glucosidase Inhibitors: Structure-Activity Relationship, Molecular Docking, and Kinetic Studies Publisher



Moghaddam FM1 ; Daneshfar M1 ; Daneshfar Z2 ; Iraji A3, 4 ; Samandarinajafabad A5 ; Faramarzi MA6 ; Mahdavi M5
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Authors Affiliations
  1. 1. Laboratory of Organic Synthesis and Natural Products, Department of Chemistry, Sharif University of Technology, Azadi Street, PO Box 111559516, Tehran, Iran
  2. 2. Department of Chemistry, Faculty of Science, K. N. Toosi University of Technology, P.O. Box 15875-4416, Tehran, Iran
  3. 3. Stem Cells Technology Research Center, Shiraz University of Medical Sciences, Shiraz, Iran
  4. 4. Central Research laboratory, Shiraz University of Medical Sciences, Shiraz, Iran
  5. 5. Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran
  6. 6. Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Tehran University of Medical Sciences, P.O. Box 14155-6451, 1417614411, Tehran, Iran

Source: Journal of Molecular Structure Published:2022


Abstract

In the present study, metal complexes of 1-amidino-O-alkylureas were designed, synthesized and characterized by elemental analyses, FT-IR spectra, XRD, Mass analyses and scanning electron microscopy (SEM). All synthesized complexes were screen as α-Glucosidase inhibitors. According to the in vitro results, the Cu (II) complexes showed superior potency compared to other tested metal complexes. Particularly, [Cu(L-Me)2](Cl)2 (1b) showed the strongest inhibition against α-Glucosidase with an IC50 value of 2.75 ± 0.3 µM which was comparable to that of acarbose (IC50 = 750 µM). These findings are supported by the ligands and enzyme interactions through molecular docking. © 2021 Elsevier B.V.
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