Synthesis and biological evaluation of phloroglucinol derivatives possessing α‐glycosidase, acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase inhibitory activity

J Biochem & Molecular Tox

et al. 2018

Self Cite

Novel substituted thiophene derivatives (1, 2a‐e, 3, and 4) were synthesized and their structures were characterized by infrared radiation, nuclear magnetic resonance, and mass analysis. These novel substituted thiophene derivatives were effective inhibitor compounds of the carbonic anhydrase I and II isozymes (hCA I and II), and acetylcholinesterase (AChE) enzyme with K i values in the range of 447.28 to 1004.65 nM for hCA I, 309.44 to 935.93 nM for hCA II, and 0.28 to 4.01 nM for AChE, respectively. Novel substituted thiophene derivatives can be good candidate drugs for the treatment of some diseases like neurological disorders, epilepsy, glaucoma, gastric and duodenal ulcers, mountain sickness, or osteoporosis as carbonic anhydrase isozymes inhibitors, and for the treatment of Alzheimer’s and Parkinson’s diseases as acetylcholinesterase inhibitors.

Section: Resultsmentioning

confidence: 99%

Synthesis and characterization of novel substituted thiophene derivatives and discovery of their carbonic anhydrase and acetylcholinesterase inhibition effects

Çetin

J Biochem & Molecular Tox

et al. 2018

Self Cite

“…This enzyme plays a key role in the digestion of starch and glycogen compounds, and is considered part of the mechanism for the treatment of disorders of metabolites. Plant cells are a significant source of chemical constituents with potential for inhibition of this metabolic enzyme and also can be used as functional food sources and therapeutics …”

Section: Introductionmentioning

confidence: 99%

Tannic acid as a natural antioxidant compound: Discovery of a potent metabolic enzyme inhibitor for a new therapeutic approach in diabetes and Alzheimer's disease

J Biochem & Molecular Tox

Saltan

2019

Self Cite

Multiple studies have been recorded on the synthesis and design of multi‐aim anti‐Alzheimer molecules. Using dual butyrylcholinesterase/acetylcholinesterase inhibitor molecules has attracted more interest in the therapy for Alzheimer's disease. In this study, a tannic acid compound showed excellent inhibitory effects against acetylcholine esterase (AChE), α‐glycosidase, α‐amylase, and butyrylcholinesterase (BChE). IC50 values of tannic acid obtained 11.9 nM against α‐glycosidase and 3.3 nM against α‐amylase, respectively. In contrast, Ki values were found of 50.96 ± 2.18 µM against AChE and 53.17 ± 4.47 µM against BChE. α‐Glycosidase inhibitor compounds can be utilized as a novel group of antidiabetic drugs. By competitively decreasing glycosidase activity, these inhibitor molecules help to hamper the fast breakdown of sugar molecules and thereby control the blood sugar level.

“…Carbonic anhydrase (CA) is an important enzyme containing metal ions in active site. It catalyzes the reversible hydration of carbon dioxide (CO 2 ) to proton (H + ) and bicarbonate (HCO − 3 ) . The CA isoforms are grouped due to the properties such as catalytic activity, tissue and dispersion, subcellular location, expression levels, kinetic properties, and inhibitor sensitivity.…”

Section: Introductionmentioning

confidence: 99%

Some pyrazoles derivatives: Potent carbonic anhydrase, α‐glycosidase, and cholinesterase enzymes inhibitors

Çetin

et al. 2018

Archiv der Pharmazie

Self Cite

A series of substituteed pyrazol‐4‐yl‐diazene derivatives were found to be effective inhibitors against α‐glycosidase, cytosolic carbonic anhydrase I and II isoforms (hCA I and II), butyrylcholinesterase (BChE), and acetylcholinesterase (AChE) with Ki values in the range of 33.72 ± 7.93 to 90.56 ± 27.52 nM for α‐glycosidase, 1.06 ± 0.16 to 9.83 ± 0.74 nM for hCA I, 0.68 ± 0.12 to 7.16 ± 1.14 nM for hCA II, 44.66 ± 10.06 to 78.34 ± 17.83 nM for AChE, and 50.36 ± 13.88 to 88.36 ± 20.03 nM for BChE, respectively. Recently, inhibition of these metabolic enzymes has been considered as a promising factor for pharmacologic intervention in a diversity of disturbances, such as diabetes, glaucoma, obesity, epilepsy, cancer, and neurodegenerative diseases.