Development of multifunctional molecules as potential therapeutic candidates for Alzheimer's disease, Parkinson's disease, and amyotrophic lateral sclerosis in the …

MG Savelieff, G Nam, J Kang, HJ Lee, M Lee… - Chemical …, 2018 - ACS Publications
Neurodegenerative diseases pose a substantial socioeconomic burden on society.
Unfortunately, the aging world population and lack of effective cures foreshadow a negative …

Inhibitory potential of nitrogen, oxygen and sulfur containing heterocyclic scaffolds against acetylcholinesterase and butyrylcholinesterase

RJ Obaid, N Naeem, EU Mughal, MM Al-Rooqi… - RSC …, 2022 - pubs.rsc.org
Heterocycles are the key structures in organic chemistry owing to their immense applications
in the biological, chemical, and pharmaceutical fields. Heterocyclic compounds perform …

Recent progress in the identification of selective butyrylcholinesterase inhibitors for Alzheimer's disease

Q Li, H Yang, Y Chen, H Sun - European journal of medicinal chemistry, 2017 - Elsevier
Alzheimer's disease (AD) is one of the most prevalent neurodegenerative disorders with
notable factor of dysfunction in cholinergic system. Low ACh level can be observed in the …

Comparison of the binding of reversible inhibitors to human butyrylcholinesterase and acetylcholinesterase: A crystallographic, kinetic and calorimetric study

TL Rosenberry, X Brazzolotto, IR Macdonald… - Molecules, 2017 - mdpi.com
Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) hydrolyze the
neurotransmitter acetylcholine and, thereby, function as coregulators of cholinergic …

8-Hydroxyquinolines in medicinal chemistry: A structural perspective

V Oliveri, G Vecchio - European journal of medicinal chemistry, 2016 - Elsevier
Hydroxyquinolines are heterocyclic compounds characterized by a moderate metal-binding
affinity. The interest in 8-hydroxyquinolines has grown exponentially in the last two decades …

Donepezil-based multi-functional cholinesterase inhibitors for treatment of Alzheimer's disease

Q Li, S He, Y Chen, F Feng, W Qu, H Sun - European journal of medicinal …, 2018 - Elsevier
Alzheimer's disease (AD) is one of the most common neurodegenerative disorders in elderly
people. Considering the multifactorial nature of AD, the concept of multi-target-directed …

The magic of crystal structure-based inhibitor optimization: development of a butyrylcholinesterase inhibitor with picomolar affinity and in vivo activity

U Kosak, B Brus, D Knez, S Zakelj… - Journal of medicinal …, 2018 - ACS Publications
The enzymatic activity of butyrylcholinesterase (BChE) in the brain increases with the
progression of Alzheimer's disease, thus classifying BChE as a promising drug target in …

Discovery and structure–activity relationships of a highly selective butyrylcholinesterase inhibitor by structure-based virtual screening

SN Dighe, GS Deora, E De la Mora… - Journal of medicinal …, 2016 - ACS Publications
Structure-based virtual screening of two libraries containing 567 981 molecules was used to
discover novel, selective BuChE inhibitors, which are potentially superior symptomatic …

Discovery of a potent dual inhibitor of acetylcholinesterase and butyrylcholinesterase with antioxidant activity that alleviates Alzheimer-like pathology in old APP/PS1 …

E Viayna, N Coquelle… - Journal of Medicinal …, 2020 - ACS Publications
The combination of the scaffolds of the cholinesterase inhibitor huprine Y and the
antioxidant capsaicin results in compounds with nanomolar potencies toward human …

Discovery and biological evaluation of a novel highly potent selective butyrylcholinsterase inhibitor

Q Li, S Xing, Y Chen, Q Liao, B Xiong… - Journal of Medicinal …, 2020 - ACS Publications
To discover novel BChE inhibitors, a hierarchical virtual screening protocol followed by
biochemical evaluation was applied. The most potent compound 8012-9656 (eq BChE …