Synthesis of novel organohalogen chalcone derivatives and screening of their molecular docking study and some enzymes inhibition effects

Burmaoğlu, Serdar; Kazancioglu, Elif Akin; Kaya, Ruya; Kazancioglu, Mustafa; Karaman, Muhammet; Algul, Oztekin; Gülçin, İlhami

doi:10.1016/j.molstruc.2020.127868

Makale Tam Makale Uluslararası 2020

Synthesis of novel organohalogen chalcone derivatives and screening of their molecular docking study and some enzymes inhibition effects

Serdar Burmaoğlu, Elif Akin Kazancioglu, Ruya Kaya, Mustafa Kazancioglu, Muhammet Karaman, Oztekin Algul, İlhami Gülçin

Journal of Molecular Structure Cilt 1208 · 15.05.2020

DOI ile aç

Özet

Chalcones and their derivatives are increasing attention due to numerous biochemical and pharmacological applications. In this study, a series of novel organohalogen chalcone derivatives (5-12) were tested towards alpha-glycosidase (alpha-Gly), acetylcholinesterase (AChE) human carbonic anhydrase I (hCA I), and carbonic anhydrase II (hCA II) enzymes. These compounds (5-12) showed K,s in ranging of 16.24 - 40.96 nM on hCA I, 29.61-67.15 nM on hCA II, 1.21-4.39 nM on AChE and 12.54-35.22 nM on alpha-glycosidase. The novel organohalogen chalcone derivatives (5-12) had effective inhibition profiles against all tested metabolic enzymes. Also, because of the enzyme inhibitory effects of the compounds (5-12), they have the potential of drug candidates to treat of some diseases including epilepsy, glaucoma, type-2 diabetes mellitus (T2DM), Alzheimer's disease (AD), and leukemia. Also, the chalcone derivatives with best inhibition score docked into the active site of indicated metabolic enzymes receptors. Bro-mobenzyle and chlorophenyl moieties of chalcone derivatives contribute to their inhibitor properties on the enzymes. (C) 2020 Published by Elsevier B.V.

Anahtar kelimeler

carbonic anhydrase Acetylcholinesterase enzyme inhibition TROUT ONCORHYNCHUS-MYKISS ERYTHROCYTES IN-VITRO ISOENZYMES I CHALCONE BIOLOGICAL EVALUATION CRYSTAL-STRUCTURE HCA I 1ST SYNTHESIS alpha-glycosidase POTENT CARBONIC-ANHYDRASE ANTICHOLINERGIC ACTIVITIES

Sürdürülebilir Kalkınma Amaçları

SKA 3: Sağlıklı Bireyler

Atıf için künye

Burmaoğlu, S., Kazancioglu, E. A., Kaya, R., Kazancioglu, M., Karaman, M., Algul, O., & Gülçin, İ. (2020). Synthesis of novel organohalogen chalcone derivatives and screening of their molecular docking study and some enzymes inhibition effects. Journal of Molecular Structure, 1208. https://doi.org/10.1016/j.molstruc.2020.127868

BibTeX

@article{burmaoglu2020-68063,
  author = {Burmaoğlu, Serdar and Kazancioglu, Elif Akin and Kaya, Ruya and Kazancioglu, Mustafa and Karaman, Muhammet and Algul, Oztekin and Gülçin, İlhami},
  title = {Synthesis of novel organohalogen chalcone derivatives and screening of their molecular docking study and some enzymes inhibition effects},
  journal = {Journal of Molecular Structure},
  year = {2020},
  volume = {1208},
  issn = {0022-2860},
  doi = {10.1016/j.molstruc.2020.127868},
  url = {https://akademik.atauni.edu.tr/yayinlar/68063-synthesis-of-novel-organohalogen-chalcone-derivatives-and-screening-of-their}
}