Cited by 225Cholinesterase and Neurodegenerative DiseasesAlzheimer's disease research and treatmentsHeterocyclic Compound Synthesis and Bioactivity

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Tacrine Derivatives and Alzheimers Disease

Tumiatti, V., Minarini, A., Bolognesi, M.L., Milelli, A., Rosini, M., Melchiorre, C.·2010·Current Medicinal Chemistry

DOI 10.2174/092986710791111206

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Abstract

To date, the pharmacotherapy of Alzheimer's disease (AD) has relied on acetylcholinesterase (AChE) inhibitors (AChEIs) and, more recently, an N-methyl-D-aspartate receptor (NMDAR) antagonist. AD is a multifactorial syndrome with several target proteins contributing to its etiology. "Multi-target-directed ligands" (MTDLs) have great potential for treating complex diseases such as AD because they can interact with multiple targets. The design of compounds that can hit more than one specific AD target thus represents an innovative strategy for AD treatment. Tacrine was the first AChEI introduced in therapy. Recent studies have demonstrated its ability to interact with different AD targets. Furthermore, numerous tacrine homo- and heterodimers have been developed with the aim of improving and enlarging its biological profile beyond its ability to act as an AChEI. Several tacrine hybrid derivatives have been designed and synthesized with the same goal. This review will focus on and summarize the last two years of research into the development of tacrine derivatives able to hit AD targets beyond simple AChE inhibition.

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N-Hydroxy-N-Propargylamide Derivatives of Ferulic Acid: Inhibitors of Cholinesterases and Monoamine Oxidases
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Behavioural effects of novel multitarget anticholinesterasic derivatives in Alzheimer’s disease
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“The various hybrid derivatives of Tacrine have been designed, synthesized, and assayed up to now [9].”
Background
Pd(II)-Catalyzed Synthesis of Alicyclic[b]-Fused Pyridines via C(sp2)–H Activation of α,β-Unsaturated N-Acetyl Hydrazones with Vinyl Azides
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Functionalized reduced graphene oxide as a useful and efficient base catalyst for the preparation of 4H ‐pyran and pyran‐like tacrine compounds and their antibacterial activity
Mirza‐Aghayan, M., Mohammadi, M., Boukherroub, R., & Ravanavard, K. (2022) · Journal of Heterocyclic Chemistry · doi:10.1002/jhet.4577 · Cited by 8
An HPLC–MS method for the quantification of new acetylcholinesterase inhibitor PC 48 (7-MEOTA-donepezil like compound) in rat plasma: Application to a pharmacokinetic study
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The Development of Small Molecule Inhibitors of Glutaminyl Cyclase and Isoglutaminyl Cyclase for Alzheimer's Disease
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Current Advances in the Synthesis and Biological Evaluation of Pharmacologically Relevant 1,2,4,5-Tetrasubstituted-1H-Imidazole Derivatives
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Design, synthesis and SAR studies of novel tacrine derivatives as potent cholinesterase inhibitors
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Neuroprotective effect of Bis(Indolyl)phenylmethane in Alzheimer’s disease rat model through inhibition of hen Lysozyme amyloid fibril-induced neurotoxicity
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“…a number of chemically synthetic compounds as dual inhibitors against both Aβ production and AChE activity have been also recently designed (da Silva et al., 2004; Rodriguez-Franco et al., 2006; Tumiatti et al., 2010; Fernandez-Bachiller et al., 2012; Xie et al., 2013; Shao et al., 2014).”
Design and Development of Cholinesterase Dual Inhibitors towards Alzheimer's Disease Treatment: A Focus on Recent Contributions from Computational and Theoretical Perspective
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Molecular docking and molecular dynamics simulation approaches for identifying new lead compounds as potential AChE inhibitors
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Design, synthesis and cholinesterase inhibitory evaluation study of fluorescent N-benzylpiperidine-4-one derivatives
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“Two types of ChE enzymes have been found in the central nervous system, namely, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) (Tumiatti et al., 2010).”
Conjugates of tacrine with aminomethylidene derivatives of ethyl acetoacetate as promising agents for the treatment of Alzheimer’s disease
Grishchenko, M. V., Махаева, Г. Ф., Burgart, Y. V., Boltneva, N. P., Рудакова, Е. В., Zhilina, E. F., Shchegolkov, E. V., Ковалева, Н. В., Serebryakova, O. G., Салоутин, В. И., et al. (2023) · Russian Chemical Bulletin · doi:10.1007/s11172-023-4111-8 · Cited by 5
Strategies for Redesigning Withdrawn Drugs to Enhance Therapeutic Efficacy and Safety: A Review
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“In the same context, redesigning withdrawn drugs is the primary aspect that can be administered as a potential drug candidate for the respective target in silico and in experimental validations [173–176].”
In silico chemical profiling and identification of neuromodulators from Curcuma amada targeting acetylcholinesterase
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“Tacrine (1,3-dihydro-2H -cyclopenta [b] quinolin-2-one) is a heterocyclic compound was discovered in 1945 as the first drug against Alzheimer’s diseases (Tumiatti et al., 2010).”
Intracellular distribution of new tacrine analogues as a potential cause of their cytotoxicity against human neuroblastoma cells SH-SY5Y
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“…and also affect other targets which are relevant to AD (Bolognesi et al. 2007; Li et al. 2007; Li et al. 2009; Marco-Contelles et al. 2009; Tumiatti et al. 2010; Rampa et al. 2011; Kozurkova et al. * Kožurková Mária maria.kozurkova@upjs.sk 1 Department of Biochemistry and Microbiology,…”
Background
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Design, Synthesis, Molecular Docking and Biological Evaluation of Donepezil Analogues as Effective Anti-Alzheimer AgentsPreprint
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Authors: Tumiatti, V., Minarini, A., Bolognesi, M. L., Milelli, A., Rosini, M., & Melchiorre, C.
Affiliations: University of Bologna (IT)
Corresponding author: Rosini, M.
Melchiorre, C.
ORCID: Tumiatti, V.
Minarini, A.
Bolognesi, M.L.
Milelli, A.
Rosini, M.
Venue: Current Medicinal Chemistry
Publisher: Bentham Science Publishers Ltd.
Published: 2010-06-01
Volume: 17
Issue: 17
Pages: 1825-1838
ISSN: 0929-8673 (ISSN-L)
DOI: 10.2174/092986710791111206
OpenAlex: W2121322934
Cited by: 225
References: 0
Citations by year: 2026: 9 · 2025: 8 · 2024: 8 · 2023: 4 · 2022: 18 · 2021: 14 · 2020: 13 · 2019: 28 · 2018: 12 · 2017: 22 · 2016: 19 · 2015: 16 · 2014: 17 · 2013: 14 · 2012: 12
FWCI: 9.92
Type: journal article
Language: en
Open access: closed
Locations: Current Medicinal Chemistry (publishedVersion)
PubMed (publishedVersion)
Archivio istituzionale della ricerca (Alma Mater Studiorum Università di Bologna) (submittedVersion)
Topics: Health Sciences › Medicine › Pharmacology (medical) › Cholinesterase and Neurodegenerative Diseases
Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Alzheimer's disease research and treatments
Physical Sciences › Chemistry › Organic Chemistry › Heterocyclic Compound Synthesis and Bioactivity
Keywords: tacrine derivatives, Alzheimer's disease, acetylcholinesterase inhibitors, multi-target-directed ligands, NMDA receptor antagonists, drug repurposing
MeSH terms: Acetylcholinesterase, Alzheimer Disease, Cholinesterase Inhibitors, Humans, Models, Molecular, Structure-Activity Relationship, Tacrine, Amyloid beta-Peptides

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Tacrine Derivatives and Alzheimers Disease

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