Synthesis of novel tris-chalcones and determination of their inhibition profiles against some metabolic enzymes
Archives of Physiology and Biochemistry, cilt.127, sa.2, ss.153-161, 2021 (SCI-Expanded, Scopus)
- 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.