Novel donepezil-like N-benzylpyridinium salt derivatives as AChE inhibitors and their corresponding dihydropyridine “bio-oxidizable” prodrugs: Synthesis, biological …

R Azzouz, L Peauger, V Gembus, ML Ţînţaş… - European journal of …, 2018 - Elsevier
As an extension of our previous work on donepezil-based “bio-oxidizable” prodrug
approach, two new classes of N-benzylpyridinium donepezil analogues in tetralone B2 and …

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 …

Rational design of carbamate-based dual binding site and central AChE inhibitors by a “biooxidisable” prodrug approach: Synthesis, in vitro evaluation and docking …

ML Ţînţaş, V Gembus, F Alix, A Barré, G Coadou… - European Journal of …, 2018 - Elsevier
Herein, we report a new class of dual binding site AChE inhibitor 4 designed to exert a
central cholinergic activation thanks to a redox-activation step of a prodrug precursor 3 …

Synthesis and biological evaluation as AChE inhibitors of new indanones and thiaindanones related to donepezil

Z Omran, T Cailly, E Lescot… - European journal of …, 2005 - Elsevier
Sixty-four new indanones and thiaindanones related to donepezil were synthesized and
evaluated in vitro as potential AChE inhibitors. Among them, 11 derivatives were found to …

Synthesis, pharmacological assessment, and molecular modeling of 6-chloro-pyridonepezils: New dual AChE inhibitors as potential drugs for the treatment of …

A Samadi, M de la Fuente Revenga, C Pérez… - European journal of …, 2013 - Elsevier
Chloro-pyridonepezils are chloropyridine–donepezil hybrids designed by combining the N-
benzylpiperidine moiety present in donepezil with the 2-chloropyridine-3, 5-dicarbonitrile …

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 …

Design, synthesis and pharmacological evaluation of N-benzyl-piperidinyl-aryl-acylhydrazone derivatives as donepezil hybrids: Discovery of novel multi-target anti …

FPD Viegas, M de Freitas Silva, MD da Rocha… - European Journal of …, 2018 - Elsevier
A new series of sixteen multifunctional N-benzyl-piperidine-aryl-acylhydrazones hybrid
derivatives was synthesized and evaluated for multi-target activities related to Alzheimer's …

Discovery of thiazole salt AChE inhibitors and development of thiamine disulfide prodrugs targeting the central nervous system

C Liu, M Zou, J Zuo, H Xie, W Lyu, J Xu, F Feng… - Bioorganic …, 2023 - Elsevier
The selective AChE inhibitor donepezil has been approved by the FDA as a first-line drug for
the treatment of mild to moderate AD. However, many peripheral side effects were observed …

Benzofuran-derived benzylpyridinium bromides as potent acetylcholinesterase inhibitors

F Baharloo, MH Moslemin, H Nadri, A Asadipour… - European journal of …, 2015 - Elsevier
A series of benzofuran-based N-benzylpyridinium derivatives 5a–o were designed and
synthesized as novel AChE inhibitors. The synthetic pathway of the compounds involved the …

Discovery of quinazolin-4 (3h)-one derivatives as novel ache inhibitors with anti-inflammatory activities

L Lv, M Maimaitiming, Y Huang, J Yang, S Chen… - European Journal of …, 2023 - Elsevier
Abstract A series of quinazolin-4 (3H)-one derivatives was designed through scaffold-
hopping strategy and synthesized as novel multifunctional anti-AD agents demonstrating …