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Synthesis, characterization, and biological studies of chalcone derivatives containing Schiff bases: Synthetic derivatives for the treatment of epilepsy and Alzheimer's disease.
- Source :
-
Archiv der Pharmazie [Arch Pharm (Weinheim)] 2020 Dec; Vol. 353 (12), pp. e2000202. Date of Electronic Publication: 2020 Aug 20. - Publication Year :
- 2020
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Abstract
- In this study, first, Schiff base-containing chalcone derivatives were synthesized. The human carbonic anhydrase (hCA) isoenzymes I and II were then purified from human erythrocytes using Sepharose-4B-l-tyrosine-sulfanilamide affinity chromatography. In addition, the inhibitory effects of the newly synthesized compounds on the activities of hCA and acetylcholinesterase (AChE) were investigated in vitro, using the esterase and acetylcholine iodide method. The IC <subscript>50</subscript> values were determined and the K <subscript>i</subscript> values of AChE and hCA activities were calculated from the Lineweaver-Burk graphs determined in this study. The hCA I isoform was inhibited by these chalcone derivatives containing Schiff bases (3a-j and 5a-f) in low nanomolar levels, whose K <subscript>i</subscript> values ranged between 141.88 ± 24.10 and 2,234.47 ± 38.11 nM. Against the physiologically dominant isoform hCA II, the compounds demonstrated K <subscript>i</subscript> values varying from 199.31 ± 40.45 to 602.79 ± 263.22 nM. Also, these compounds effectively inhibited AChE, with K <subscript>i</subscript> values ranging from 20.41 ± 6.04 to 125.94 ± 23.88 nM. According to these results, the newly synthesized molecules were found to be potent inhibitors of these enzymes.<br /> (© 2020 Deutsche Pharmazeutische Gesellschaft.)
- Subjects :
- Acetylcholinesterase metabolism
Alzheimer Disease enzymology
Alzheimer Disease psychology
Anticonvulsants chemical synthesis
Carbonic Anhydrase I metabolism
Carbonic Anhydrase II metabolism
Carbonic Anhydrase Inhibitors chemical synthesis
Chalcones chemical synthesis
Cholinesterase Inhibitors chemical synthesis
Drug Design
Erythrocytes enzymology
GPI-Linked Proteins antagonists & inhibitors
GPI-Linked Proteins metabolism
Molecular Structure
Schiff Bases
Structure-Activity Relationship
Alzheimer Disease drug therapy
Anticonvulsants pharmacology
Carbonic Anhydrase I antagonists & inhibitors
Carbonic Anhydrase II antagonists & inhibitors
Carbonic Anhydrase Inhibitors pharmacology
Chalcones pharmacology
Cholinesterase Inhibitors pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1521-4184
- Volume :
- 353
- Issue :
- 12
- Database :
- MEDLINE
- Journal :
- Archiv der Pharmazie
- Publication Type :
- Academic Journal
- Accession number :
- 32815568
- Full Text :
- https://doi.org/10.1002/ardp.202000202