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Tacrine Derivatives and Alzheimers Disease
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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“In spite of that, thanks to its low-molecular weight and high synthetic accessibility, 16 has been widely exploited as a starting fragment of hybrids able to combine AChE inhibition with other additional effects and endowed with reduced hepatotoxicity.91”
From From combinations to multitarget-directed ligands: A continuum in Alzheimer’s disease polypharmacology (2021) · cites this paper as [91]
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New Acetylcholinesterase Inhibitors for Alzheimer's Disease
Mehta, M., Adem, A., & Sabbagh, M. N. (2011) · International Journal of Alzheimer s Disease · doi:10.1155/2012/728983 · Cited by 436
“Eventually, tacrine was discontinued due to the aforementioned liver toxicity which was thought to be caused by the affinity for BuChE [2] and because less toxic, better tolerated drugs with easier dosing schedule were approved.”
BackgroundCHOLINESTERASES, A TARGET OF PHARMACOLOGY AND TOXICOLOGY
Pohanka, M. (2011) · Biomedical Papers · doi:10.5507/bp.2011.036 · Cited by 377
Molecular Hybridization as a Tool for Designing Multitarget Drug Candidates for Complex Diseases
Ivasiv, V., Albertini, C., Gonçalves, A. E., Rossi, M., & Bolognesi, M. L. (2019) · Current Topics in Medicinal Chemistry · doi:10.2174/1568026619666190619115735 · Cited by 396
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Metadata
- 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.
- 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)
- 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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