Synthesis of novel tris-chalcones and determination of their inhibition profiles against some metabolic enzymes.
Archives of physiology and biochemistry, cilt.127, ss.153-161, 2021 (SCI-Expanded, Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 127
- 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
- Erzincan Binali Yıldırım Üniversitesi Adresli: Evet
Özet
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 alpha-glycosidase (alpha-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 alpha-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.