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Novel Quinazolin–Sulfonamid Derivatives: Synthesis, Characterization, Biological Evaluation, and Molecular Docking Studies Publisher Pubmed



Sepehri N1 ; Mohammadikhanaposhtani M2 ; Asemanipoor N3 ; Hosseini S4 ; Biglar M3 ; Larijani B3 ; Mahdavi M3 ; Hamedifar H5 ; Taslimi P6 ; Sadeghian N7 ; Norizadehtazehkand M8 ; Gulcin I7
Authors
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Authors Affiliations
  1. 1. Nano Alvand Company, Avicenna Tech Park, Tehran University of Medical Sciences, Tehran, Iran
  2. 2. Cellular and Molecular Biology Research Center, Health Research Institute, Babol University of Medical Sciences, Babol, Iran
  3. 3. Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran
  4. 4. Shahid Beheshti University of Medical Sciences, Tehran, Iran
  5. 5. CinnaGen Medical Biotechnology Research Center, Alborz University of Medical Sciences, Karaj, Iran
  6. 6. Department of Biotechnology, Faculty of Science, Bartin University, Bartin, Turkey
  7. 7. Department of Chemistry, Faculty of Science, Ataturk University, Erzurum, Turkey
  8. 8. Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Zonguldak Bulent Ecevit University, Zonguldak, Turkey

Source: Journal of Biomolecular Structure and Dynamics Published:2022


Abstract

In the design of novel drugs, the formation of hybrid molecules via the combination of several pharmacophores can give rise to compounds with interesting biochemical profiles. A series of novel quinazolin–sulfonamid derivatives (9a–m) were synthesized, characterized and evaluated for their in vitro antidiabetic, anticholinergics, and antiepileptic activity. These synthesized novel quinazolin–sulfonamid derivatives (9a–m) were found to be effective inhibitor molecules for the α-glycosidase, human carbonic anhydrase I and II (hCA I and hCA II), butyrylcholinesterase (BChE) and acetylcholinesterase (AChE) enzyme, with Ki values in the range of 100.62 ± 13.68–327.94 ± 58.21 nM for α-glycosidase, 1.03 ± 0.11–14.87 ± 2.63 nM for hCA I, 1.83 ± 0.24–15.86 ± 2.57 nM for hCA II, 30.12 ± 3.81–102.16 ± 13.87 nM for BChE, and 26.16 ± 3.63–88.52 ± 20.11 nM for AChE, respectively. In the last step, molecular docking calculations were made to compare biological activities of molecules against enzymes which are achethylcholinesterase, butyrylcholinesterase and α-glycosidase. Communicated by Ramaswamy H. Sarma. © 2020 Informa UK Limited, trading as Taylor & Francis Group.
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