Piperidine derivatives: recent advances in synthesis and pharmacological applications

NA Frolov, AN Vereshchagin - International Journal of Molecular Sciences, 2023 - mdpi.com
Piperidines are among the most important synthetic fragments for designing drugs and play
a significant role in the pharmaceutical industry. Their derivatives are present in more than …

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 …

Molecular chameleons in drug discovery

V Poongavanam, LHE Wieske, S Peintner… - Nature Reviews …, 2024 - nature.com
Molecular chameleons possess a flexibility that allows them to dynamically shield or expose
polar functionalities in response to the properties of the environment. Although the concept …

[HTML][HTML] From tryptophan-based amides to tertiary amines: Optimization of a butyrylcholinesterase inhibitor series

A Meden, D Knez, X Brazzolotto, F Nachon… - European journal of …, 2022 - Elsevier
Lead optimization of a series of tryptophan-based nanomolar butyrylcholinesterase (BChE)
inhibitors led to tertiary amines as highly potent, achiral, sp 3-rich analogues with better …

Design, synthesis, and biological evaluation of aromatic tertiary amine derivatives as selective butyrylcholinesterase inhibitors for the treatment of Alzheimer's disease

X Lu, N Qin, Y Liu, C Du, F Feng, W Liu, Y Chen… - European Journal of …, 2022 - Elsevier
Butyrylcholinesterase (BChE) is recently regarded as a biomarker in progressed Alzheimer's
disease (AD), the development of selective BChE inhibitors has attracted a great deal of …

Exploiting butyrylcholinesterase inhibitors through a combined 3-D pharmacophore modeling, QSAR, molecular docking, and molecular dynamics investigation

S Kumar, A Manoharan, J Jayalakshmi… - RSC …, 2023 - pubs.rsc.org
Alzheimer's disease (AD), a neurodegenerative condition associated with ageing, can occur.
AD gradually impairs memory and cognitive function, which leads to abnormal behavior …

Advances in screening assays for identifying cholinesterase ligands

PCO de Oliveira, LW Tinoco, CL Cardoso… - TrAC Trends in …, 2023 - Elsevier
Acetylcholinesterase and butyrylcholinesterase are the two enzymes involved in the
cholinergic system and its modulation. These enzymes have been recognized as …

Contemporary medicinal-chemistry strategies for the discovery of selective butyrylcholinesterase inhibitors

L Jing, G Wu, D Kang, Z Zhou, Y Song, X Liu… - Drug discovery today, 2019 - Elsevier
Highlights•BChE is considered a promising drug target for the treatment of moderate to
severe Alzheimer's disease.•The development of selective BChE inhibitors will move on …

Discovery of δ-sultone-fused pyrazoles for treating Alzheimer's disease: Design, synthesis, biological evaluation and SAR studies

Y Xu, Z Zhang, X Jiang, X Chen, Z Wang… - European Journal of …, 2019 - Elsevier
A class of novel δ-sulfonolactone-fused pyrazole scaffold was prepared via sulfur (VI)
fluoride exchange (SuFEx) chemistry using aryl sulfonyl fluorides and pyrazolones. Enzyme …

Overview of novel multifunctional agents based on conjugates of γ-carbolines, carbazoles, tetrahydrocarbazoles, phenothiazines, and aminoadamantanes for …

GF Makhaeva, EF Shevtsova, NP Boltneva… - Chemico-Biological …, 2019 - Elsevier
Alzheimer's disease (AD) is a multifactorial neurodegenerative process whose effective
treatment will require drugs that can act simultaneously on multiple pathogenic targets …