Discovery of potential pancreatic cholesterol esterase inhibitors using pharmacophore modelling, virtual screening, and optimization studies

S John, S Thangapandian, S Sakkiah… - Journal of enzyme …, 2011 - Taylor & Francis
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 …

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 …

[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 …

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 …

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 …

Cholinesterase inhibitory activities of some flavonoid derivatives and chosen xanthone and their molecular docking studies

MTH Khan, I Orhan, FS Şenol, M Kartal, B Şener… - Chemico-Biological …, 2009 - Elsevier
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 …

New cholesterol esterase inhibitors based on rhodanine and thiazolidinedione scaffolds

S Heng, W Tieu, S Hautmann, K Kuan… - Bioorganic & medicinal …, 2011 - Elsevier
We present a new class of inhibitors of pancreatic cholesterol esterase (CEase) based on
'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 …

Design, synthesis and docking study of novel coumarin ligands as potential selective acetylcholinesterase inhibitors

F Sonmez, B Zengin Kurt, I Gazioglu… - Journal of enzyme …, 2017 - Taylor & Francis
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 …

Cholinesterase inhibition activity and molecular docking study of eugenol derivatives

KM Zamli, A Asari, KY Khaw, V Murugaiyah… - Sains …, 2021 - research.monash.edu
The study was conducted to explore the anticholinesterase inhibition property of eugenol
derived molecules. Ten eugenol derivatives were synthesized and evaluated for the …