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Makale Tam Makale Uluslararası 2023

Metal-Free Synthesis via Intramolecular Cyclization, Enzyme Inhibition Properties and Molecular Docking of Novel Isoindolinones

Ufuk Atmaca, Ruya Saglamtas, Yusuf Sert, Murat Çelik, İlhami Gülçin

ChemistrySelect Cilt 8 · Sayı 9 · 06.03.2023
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Özet

Highly effective one-pot synthesis of novel isoindolinones from various 2-benzoylbenzoic acid derivatives with intramolecular cyclization in the presence of chlorosulfonyl isocyanate was reported in mild conditions in the absence a metal catalyst. Novel synthesized compounds were tested against some metabolic enzymes including acetylcholinesterase (AChE), butyrylcholinesterase (BChE), α-glycosidase and carbonic anhydrase I and II (hCA I and hCA II) enzymes that associated with Alzheimer's disease (AD), type-2 diabetes mellitus (T2DM), epilepsy, and glaucoma. A series of novel isoindolinones (2 a–l) were evaluated as highly potent inhibition ability toward AChE (Kis: 2.33–13.81 μM), BChE (Kis: 1.45–12.27 μM), α-glycosidase (Kis: 8.03–23.05 μM), hCA I (Kis: 2.23–17.35 μM) and hCA II (Kis: 2.86–18.13 μM). Also, for these inhibitors, in silico molecular docking simulations and calculations were done with the Autodock Vina program to support the in vitro experimental studies.

Anahtar kelimeler

carbonic anhydrase DERIVATIVES Acetylcholinesterase Butyrylcholinesterase TROUT ONCORHYNCHUS-MYKISS ISOENZYMES I BIOLOGICAL EVALUATION CRYSTAL-STRUCTURE CARBONIC-ANHYDRASE INHIBITION ERYTHROCYTE ISOZYMES I alpha-glycosidase α-glycosidase ALPHA-GLUCOSIDASE INHIBITORS Isoindolinone Sulfamate

Sürdürülebilir Kalkınma Amaçları

  • SKA 3: Sağlıklı Bireyler
  • SKA 7: Erişilebilir ve Temiz Enerji
  • SKA 8: İnsana Yakışır İş ve Ekonomik Büyüme
  • SKA 9: Sanayi, Yenilikçilik ve Altyapı
  • SKA 13: İklim Eylemi
  • SKA 17: Amaçlar için Ortaklıklar

Atıf için künye

Atmaca, U., Saglamtas, R., Sert, Y., Çelik, M., & Gülçin, İ. (2023). Metal-Free Synthesis via Intramolecular Cyclization, Enzyme Inhibition Properties and Molecular Docking of Novel Isoindolinones. ChemistrySelect, 8(9). https://doi.org/10.1002/slct.202204578

BibTeX 
@article{atmaca2023-67779,
  author = {Atmaca, Ufuk and Saglamtas, Ruya and Sert, Yusuf and Çelik, Murat and Gülçin, İlhami},
  title = {Metal-Free Synthesis via Intramolecular Cyclization, Enzyme Inhibition Properties and Molecular Docking of Novel Isoindolinones},
  journal = {ChemistrySelect},
  year = {2023},
  volume = {8},
  number = {9},
  issn = {2365-6549},
  doi = {10.1002/slct.202204578},
  url = {https://akademik.atauni.edu.tr/yayinlar/67779-metal-free-synthesis-via-intramolecular-cyclization-enzyme-inhibition-properties}
}