The New Acetylcholinesterase Inhibitors PC‐37 and PC‐48 (7‐Methoxytacrine‐Donepezil‐Like Compounds): Characterization of Their Metabolites in Human Liver …

J Zdarova Karasova, M Mzik, M Hroch… - Basic & Clinical …, 2018 - Wiley Online Library
The objective of this study was to elucidate the pharmacokinetics and metabolite formation
of newly developed non‐selective AC hE/BC hE 7‐MEOTA‐donepezil‐like inhibitors for …

An HPLC–MS method for the quantification of new acetylcholinesterase inhibitor PC 48 (7-MEOTA-donepezil like compound) in rat plasma: Application to a …

M Mzik, J Korabecny, E Nepovimova, V Voříšek… - … of Chromatography B, 2016 - Elsevier
A simple, rapid and sensitive method based on liquid chromatography–tandem mass
spectrometry (LC–MS/MS) has been developed and validated for the quantitative …

Synthesis of new donepezil analogues and investigation of their effects on cholinesterase enzymes

BN Sağlık, S Ilgın, Y Özkay - European journal of medicinal chemistry, 2016 - Elsevier
Abstract Donepezil (DNP), an acetylcholinesterase (AChE) inhibitor, is one of the most
preferred choices in Alzheimer diseases (AD) therapy. In the present study, 38 new DNP …

Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease

ZM Wang, P Cai, QH Liu, DQ Xu, XL Yang… - European Journal of …, 2016 - Elsevier
A series of novel donepezil derivatives was designed, synthesized and evaluated as
multifunctional acetylcholinesterase (AChE) inhibitors for the treatment of Alzheimer's …

Synthesis and pharmacological evaluation of donepezil-based agents as new cholinesterase/monoamine oxidase inhibitors for the potential application against …

F Li, ZM Wang, JJ Wu, J Wang, SS Xie… - Journal of enzyme …, 2016 - Taylor & Francis
In a continuing effort to develop multitargeted compounds as potential treatment agents
against Alzheimer's disease (AD), a series of donepezil-like compounds were designed …

Inhibitory effect of orally administered donepezil hydrochloride (E2020), a novel treatment for Alzheimer's disease, on cholinesterase activity in rats

T Kosasa, Y Kuriya, K Matsui, Y Yamanishi - European journal of …, 2000 - Elsevier
Donepezil hydrochloride ((±)-2-[(1-benzylpiperidin-4-yl) methyl]-5, 6-dimethoxy-indan-1-one
monohydrochloride: E2020: donepezil) is a potent and selective acetylcholinesterase …

Pyridonepezils, new dual AChE inhibitors as potential drugs for the treatment of Alzheimer's disease: Synthesis, biological assessment, and molecular modeling

A Samadi, M Estrada, C Pérez… - European journal of …, 2012 - Elsevier
The synthesis, biological assessment and molecular modeling of new pyridonepezils1–8,
able to inhibit human acetylcholinesterase (hAChE) and human butyrylcholinesterase …

Targeting Alzheimer's disease by investigating previously unexplored chemical space surrounding the cholinesterase inhibitor donepezil

DG van Greunen, W Cordier, M Nell… - European Journal of …, 2017 - Elsevier
A series of twenty seven acetylcholinesterase inhibitors, as potential agents for the treatment
of Alzheimer's disease, were designed and synthesised based upon previously unexplored …

Donepezil-based central acetylcholinesterase inhibitors by means of a “bio-oxidizable” prodrug strategy: design, synthesis, and in vitro biological evaluation

L Peauger, R Azzouz, V Gembus… - Journal of medicinal …, 2017 - ACS Publications
With the aim of reducing side effects of acetylcholinesterase inhibitors (AChEIs) during
symptomatic treatment of Alzheimer's disease, we report herein a new class of donepezil …

Multifunctional donepezil analogues as cholinesterase and BACE1 inhibitors

KD Green, MY Fosso, S Garneau-Tsodikova - Molecules, 2018 - mdpi.com
A series of 22 donepezil analogues were synthesized through alkylation/benzylation and
compared to donepezil and its 6-O-desmethyl adduct. All the compounds were found to be …