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

Burmaoglu S., YILMAZ A. O., POLAT M., Kaya R., GÜLÇİN İ., Algul O.

Archives of Physiology and Biochemistry, cilt.127, sa.2, ss.153-161, 2021 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 127 Sayı: 2
  • Basım Tarihi: 2021
  • Doi Numarası: 10.1080/13813455.2019.1623265
  • Dergi Adı: Archives of Physiology and Biochemistry
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, BIOSIS, CAB Abstracts, Chemical Abstracts Core, EMBASE, Food Science & Technology Abstracts, MEDLINE, Veterinary Science Database
  • Sayfa Sayıları: ss.153-161
  • Anahtar Kelimeler: Tris-chalcone, carbonic anhydrase, acetylcholinesterase, butyrylcholinesterase, alpha-glycosidase, CARBONIC-ANHYDRASE INHIBITORS, TROUT ONCORHYNCHUS-MYKISS, ERYTHROCYTE ISOZYMES I, CRYSTAL-STRUCTURE, ANTICHOLINERGIC ACTIVITIES, BIOLOGICAL EVALUATION, MEDICINAL CHEMISTRY, 1ST SYNTHESIS, HALOGEN BOND, ACETYLCHOLINESTERASE
  • Atatürk Üniversitesi Adresli: Evet

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.