Synthesis of novel tris-chalcones and determination of their inhibition profiles against some metabolic enzymes

Burmaoglu, Serdar; YILMAZ, Ali Osman; POLAT, MUHAMMED; Kaya, Ruya; Gülçin, İlhami; Algul, Oztekin

doi:10.1080/13813455.2019.1623265

Makale Tam Makale Uluslararası 2021

Synthesis of novel tris-chalcones and determination of their inhibition profiles against some metabolic enzymes

Serdar Burmaoglu, Ali Osman YILMAZ, MUHAMMED POLAT, Ruya Kaya, İlhami Gülçin, Oztekin Algul

ARCHIVES OF PHYSIOLOGY AND BIOCHEMISTRY Cilt 127 · Sayı 2 · ss. 153–161 · 01.01.2021

DOI ile aç

Özet

© 2019 Informa UK Limited, trading as Taylor & Francis Group.In this study, we report the synthesis of novel tris-chalcones and testing of human carbonic anhydrase I, and II isoenzymes (hCA I, and hCA II), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and α-glycosidase (α-Gly) inhibitors for the development of novel chalcone structures towards for treatment of some diseases. The compounds demonstrated K i values between 13.6 ± 1.1 and 50.0 ± 17.1 nM on hCA I, 9.9 ± 0.8 and 39.5 ± 15.1 nM on hCA II, 3.1 ± 0.2 and 20.1 ± 1.9 nM on AChE, 4.9 ± 0.4 and 14.7 ± 5.2 nM on BChE and 3.9 ± 0.2 and 22.4 ± 10.7 nM on α-Gly enzymes. The results revealed that novel tris-chalcones can have promising drug potential for glaucoma, leukaemia, epilepsy; Alzheimer’s disease that was associated with the high enzymatic activity of hCA I, hCA II, AChE, and BChE enzymes.

Anahtar kelimeler

carbonic anhydrase Acetylcholinesterase Butyrylcholinesterase TROUT ONCORHYNCHUS-MYKISS BIOLOGICAL EVALUATION CRYSTAL-STRUCTURE MEDICINAL CHEMISTRY CARBONIC-ANHYDRASE INHIBITORS ERYTHROCYTE ISOZYMES I 1ST SYNTHESIS alpha-glycosidase α-glycosidase ANTICHOLINERGIC ACTIVITIES Tris-chalcone HALOGEN BOND

Sürdürülebilir Kalkınma Amaçları

SKA 3: Sağlıklı Bireyler

Atıf için künye

Burmaoglu, S., YILMAZ, A. O., POLAT, M., Kaya, R., Gülçin, İ., & Algul, O. (2021). Synthesis of novel tris-chalcones and determination of their inhibition profiles against some metabolic enzymes. ARCHIVES OF PHYSIOLOGY AND BIOCHEMISTRY, 127(2), 153–161. https://doi.org/10.1080/13813455.2019.1623265

BibTeX

@article{burmaoglu2021-67885,
  author = {Burmaoglu, Serdar and YILMAZ, Ali Osman and POLAT, MUHAMMED and Kaya, Ruya and Gülçin, İlhami and Algul, Oztekin},
  title = {Synthesis of novel tris-chalcones and determination of their inhibition profiles against some metabolic enzymes},
  journal = {ARCHIVES OF PHYSIOLOGY AND BIOCHEMISTRY},
  year = {2021},
  volume = {127},
  number = {2},
  pages = {153--161},
  issn = {1381-3455},
  doi = {10.1080/13813455.2019.1623265},
  url = {https://akademik.atauni.edu.tr/yayinlar/67885-synthesis-of-novel-tris-chalcones-and-determination-of-their-inhibition-profiles}
}