Discovery of potential pancreatic cholesterol esterase inhibitors using pharmacophore modelling, virtual screening, and optimization studies
Pancreatic cholesterol esterase (CEase) is a serine hydrolase involved in the hydrolysis of
variety of lipids and transport of free cholesterol. In this study, pharmacophore hypotheses …
variety of lipids and transport of free cholesterol. In this study, pharmacophore hypotheses …
Design, synthesis and biological evaluation of biguanids and biguanid-sulfonamides as cholinesterase inhibitors
Ö Güngör, M Köse - Journal of Molecular Structure, 2022 - Elsevier
Recently, the inhibitory impact of enzymes acetylcholinesterase (AChE) and
butyrylcholinesterase (BChE) have emerged as a hopeful approach for pharmacological …
butyrylcholinesterase (BChE) have emerged as a hopeful approach for pharmacological …
[HTML][HTML] Novel acetylcholinesterase inhibitors: Synthesis, docking and inhibitory activity evaluation of 4-benzamido-N-(1-benzylpiperidin-4-yl) benzamide derivatives
A Mohammadi-Farani, S Nazari, M Mohammadi… - Results in …, 2024 - Elsevier
The cholinergic hypothesis is one of the basic approaches for designing and discovering
novel anti-Alzheimer drugs. Application of the pharmacophore of well-known drugs like …
novel anti-Alzheimer drugs. Application of the pharmacophore of well-known drugs like …
Exploring structure-activity relationship in tacrine-squaramide derivatives as potent cholinesterase inhibitors
B Svobodova, E Mezeiova, V Hepnarova, M Hrabinova… - Biomolecules, 2019 - mdpi.com
Tacrine was the first drug to be approved for Alzheimer's disease (AD) treatment, acting as a
cholinesterase inhibitor. The neuropathological hallmarks of AD are amyloid-rich senile …
cholinesterase inhibitor. The neuropathological hallmarks of AD are amyloid-rich senile …
Discovery of novel cholinesterase inhibitors easily crossing the blood‐brain barrier via structure‐property relationship investigation: Methylenedioxy‐cinnamicamides …
HR Liu, Q Shi, ZY Yang, YH Wang, BX Yi… - Chemistry & …, 2024 - Wiley Online Library
In the present investigation, a series of dimethoxy or methylenedioxy substituted‐
cinnamamide derivatives containing tertiary amine moiety (N. N‐Dimethyl, N, N‐diethyl …
cinnamamide derivatives containing tertiary amine moiety (N. N‐Dimethyl, N, N‐diethyl …
Cholinesterase inhibitory activities of some flavonoid derivatives and chosen xanthone and their molecular docking studies
Flavonoids are one of the largest classes of plant secondary metabolites and are known to
possess a number of significant biological activities for human health. In this study, we …
possess a number of significant biological activities for human health. In this study, we …
New cholesterol esterase inhibitors based on rhodanine and thiazolidinedione scaffolds
We present a new class of inhibitors of pancreatic cholesterol esterase (CEase) based on
'priviledged'5-benzylidenerhodanine and 5-benzylidene-2, 4-thiazolidinedione structural …
'priviledged'5-benzylidenerhodanine and 5-benzylidene-2, 4-thiazolidinedione structural …
Natural inhibitors of cholinesterases: chemistry, structure–activity and methods of their analysis
N Smyrska-Wieleba, T Mroczek - International Journal of Molecular …, 2023 - mdpi.com
This article aims to provide an updated description and comparison of the data currently
available in the literature (from the last 15 years) on the studied natural inhibitors of …
available in the literature (from the last 15 years) on the studied natural inhibitors of …
Design, synthesis and docking study of novel coumarin ligands as potential selective acetylcholinesterase inhibitors
New coumaryl-thiazole derivatives with the acetamide moiety as a linker between the alkyl
chains and/or the heterocycle nucleus were synthesized and in vitro tested as …
chains and/or the heterocycle nucleus were synthesized and in vitro tested as …
Cholinesterase inhibition activity and molecular docking study of eugenol derivatives
The study was conducted to explore the anticholinesterase inhibition property of eugenol
derived molecules. Ten eugenol derivatives were synthesized and evaluated for the …
derived molecules. Ten eugenol derivatives were synthesized and evaluated for the …