Synthesis of novel organohalogen chalcone derivatives and screening of their molecular docking study and some enzymes inhibition effects
Journal of Molecular Structure, cilt.1208, 2020 (SCI-Expanded, Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 1208
- Basım Tarihi: 2020
- Doi Numarası: 10.1016/j.molstruc.2020.127868
- Dergi Adı: Journal of Molecular Structure
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, Chimica, Compendex, INSPEC
- Anahtar Kelimeler: Chalcone, Enzyme inhibition, Carbonic anhydrase, Acetylcholinesterase, alpha-Glycosidase, POTENT CARBONIC-ANHYDRASE, TROUT ONCORHYNCHUS-MYKISS, ERYTHROCYTES IN-VITRO, CRYSTAL-STRUCTURE, 1ST SYNTHESIS, ISOENZYMES I, ANTICHOLINERGIC ACTIVITIES, BIOLOGICAL EVALUATION, ALPHA-GLYCOSIDASE, HCA I
- Atatürk Üniversitesi Adresli: Evet
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.