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Diphenyl-Substituted Triazine Derivatives: Synthesis, Α-Glucosidase Inhibitory Activity, Kinetics and in Silico Studies Publisher Pubmed



Shamim S1 ; Khan KM1, 2 ; Ali M1 ; Mahdavi M3 ; Salar U4 ; Mohammadikhanaposhtani M5 ; Faramarzi MA6 ; Ullah N7 ; Taha M2
Authors
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Authors Affiliations
  1. 1. HEJ Research Institute of Chemistry, International Center for Chemical & Biological Sciences, University of Karachi, Karachi, 75270, Pakistan
  2. 2. Department of Clinical Pharmacy, Institute for Research & Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, PO Box 31441, Dammam, Saudi Arabia
  3. 3. Endocrinology & Metabolism Research Center, Endocrinology & Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran
  4. 4. Dr. Panjwani Center for Molecular Medicine & Drug Research, International Center for Chemical & Biological Sciences, University of Karachi, Karachi, 75270, Pakistan
  5. 5. Cellular & Molecular Biology Research Center, Health Research Institute, Babol University of Medical Sciences, Babol, Iran
  6. 6. Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  7. 7. Chemistry Department, King Fahd University of Petroleum & Minerals, Dhahran, 31261, Saudi Arabia

Source: Future Medicinal Chemistry Published:2023


Abstract

Background: Diabetes mellitus (DM) is a chronic disorder, considered to be a major global health challenge in the 21st century. α-Glucosidase enzyme is a well-known drug target to treat Type II DM. Methods: A new library of biphenyl-substituted triazines was synthesized and confirmed by various spectroscopic techniques. Results: All compounds showed potent α-glucosidase inhibitory activity, with IC50 values ranging from 35.35 ± 0.34 to 564.41 ± 0.91 μM, as the standard acarbose, IC50 value of 750.7 ± 0.13 μM. Our in silico study has predicted key interactions with the enzyme's active site. Drug-likeness and absorption, distribution, metabolism, excretion and toxicity were also studied. Conclusion: This study has identified a range of potential hits against the α-glucosidase enzyme that may serve as antidiabetic agents after further investigations. © 2023 Newlands Press.