Relevant bibliographies by topics / Multi-target directed ligands (MTDLs)

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  1. Journal articles
  2. Dissertations / Theses
  3. Book chapters
  4. Conference papers

Academic literature on the topic 'Multi-target directed ligands (MTDLs)'

Author: Grafiati
Published: 5 June 2025
Last updated: 2 August 2025

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Journal articles on the topic "Multi-target directed ligands (MTDLs)"

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Pachón-Angona, Irene, Paul J. Bernard, Alexey Simakov, et al. "Design and Synthesis of Multi-Functional Ligands through Hantzsch Reaction: Targeting Ca2+ Channels, Activating Nrf2 and Possessing Cathepsin S Inhibitory, and Antioxidant Properties." Pharmaceutics 16, no. 1 (2024): 121. http://dx.doi.org/10.3390/pharmaceutics16010121.

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This work relates to the design and synthesis of a series of novel multi-target directed ligands (MTDLs), i.e., compounds 4a–l, via a convenient one-pot three-component Hantzsch reaction. This approach targeted calcium channel antagonism, antioxidant capacity, cathepsin S inhibition, and interference with Nrf2 transcriptional activation. Of these MTDLs, 4i emerged as a promising compound, demonstrating robust antioxidant activity, the ability to activate Nrf2-ARE pathways, as well as calcium channel blockade and cathepsin S inhibition. Dihydropyridine 4i represents the first example of an MTDL
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Kareem, Rzgar Tawfeeq, Fahimeh Abedinifar, Evan Abdolkareem Mahmood, Abdol Ghaffar Ebadi, Fatemeh Rajabi, and Esmail Vessally. "The recent development of donepezil structure-based hybrids as potential multifunctional anti-Alzheimer's agents: highlights from 2010 to 2020." RSC Advances 11, no. 49 (2021): 30781–97. http://dx.doi.org/10.1039/d1ra03718h.

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Singh, Manjinder, and Om Silakari. "Design, synthesis and biological evaluation of novel 2-phenyl-1-benzopyran-4-one derivatives as potential poly-functional anti-Alzheimer's agents." RSC Advances 6, no. 110 (2016): 108411–22. http://dx.doi.org/10.1039/c6ra17678j.

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Abatematteo, Francesca Serena, Mauro Niso, Marialessandra Contino, Marcello Leopoldo та Carmen Abate. "Multi-Target Directed Ligands (MTDLs) Binding the σ1 Receptor as Promising Therapeutics: State of the Art and Perspectives". International Journal of Molecular Sciences 22, № 12 (2021): 6359. http://dx.doi.org/10.3390/ijms22126359.

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The sigma-1 (σ1) receptor is a ‘pluripotent chaperone’ protein mainly expressed at the mitochondria–endoplasmic reticulum membrane interfaces where it interacts with several client proteins. This feature renders the σ1 receptor an ideal target for the development of multifunctional ligands, whose benefits are now recognized because several pathologies are multifactorial. Indeed, the current therapeutic regimens are based on the administration of different classes of drugs in order to counteract the diverse unbalanced physiological pathways associated with the pathology. Thus, the multi-targete
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Bhatia, Rohit, Sankha S. Chakrabarti, Upinder Kaur, Gaurav Parashar, Anindita Banerjee, and Ravindra K. Rawal. "Multi-Target Directed Ligands (MTDLs): Promising Coumarin Hybrids for Alzheimer’s Disease." Current Alzheimer Research 18, no. 10 (2021): 802–30. http://dx.doi.org/10.2174/1567205018666211208140551.

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Alzheimer’s disease (AZD) is an age-associated neurodegenerative disorder and is one of the common health issues around the globe. It is characterized by memory loss and a decline in other cognitive domains, including executive function. The progression of AZD is associated with complex events, and the exact pathogenesis is still unrevealed. Various mechanisms which are thought to be associated with the initiation of AZD include a decreased concentration of acetylcholine (ACh), deposition of amyloid-β (Aβ) peptide, dyshomeostasis of redox metal ions, and prolonged oxidative stress. Due to the
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Mezeiova, Eva, Lukas Prchal, Martina Hrabinova, et al. "Morphing cholinesterase inhibitor amiridine into multipotent drugs for the treatment of Alzheimer's disease." Biomedicine & Pharmacotherapy 173 (March 15, 2024): 116399. https://doi.org/10.1016/j.biopha.2024.116399.

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The search for novel drugs to address the medical needs of Alzheimer’s disease (AD) is an ongoing process relying on the discovery of disease-modifying agents. Given the complexity of the disease, such an aim can be pursued by developing so-called multi-target directed ligands (MTDLs) that will impact the disease pathophysiology more comprehensively. Herewith, we contemplated the therapeutic efficacy of an amiridine drug acting as a cholinesterase inhibitor by converting it into a novel class of novel MTDLs. Applying the linking approach, we have paired amiridine
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Bianco, Maria da Conceição Avelino Dias, Debora Inacio Leite, Frederico Silva Castelo Branco, et al. "The Use of Zidovudine Pharmacophore in Multi-Target-Directed Ligands for AIDS Therapy." Molecules 27, no. 23 (2022): 8502. http://dx.doi.org/10.3390/molecules27238502.

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The concept of polypharmacology embraces multiple drugs combined in a therapeutic regimen (drug combination or cocktail), fixed dose combinations (FDCs), and a single drug that binds to different targets (multi-target drug). A polypharmacology approach is widely applied in the treatment of acquired immunodeficiency syndrome (AIDS), providing life-saving therapies for millions of people living with HIV. Despite the success in viral load suppression and patient survival of combined antiretroviral therapy (cART), the development of new drugs has become imperative, owing to the emergence of resist
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de Freitas Silva, Matheus, Kris Simone Tranches Dias, Vanessa Silva Gontijo, Cindy Juliet Cristancho Ortiz, and Claudio Viegas. "Multi-Target Directed Drugs as a Modern Approach for Drug Design Towards Alzheimer’s Disease: An Update." Current Medicinal Chemistry 25, no. 29 (2018): 3491–525. http://dx.doi.org/10.2174/0929867325666180111101843.

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Alzheimer’s disease (AD) is a progressive multifactorial neurodegenerative disorder. Currently, no effective treatment is available and this is due to multiple factors involved in pathophysiology and severity of AD. A recent approach for the rational design of new drug candidates, also called multitarget-directed ligands (MTDL) strategy, has been used to develop a variety of hybrid compounds capable to act simultaneously in diverse biological targets. The discovery of drug candidates capable of targeting multiple factors involved in AD pathogenesis would greatly facilitate in improving therape
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Azam, Uzma, Muhammad Moazzam Naseer, and Christophe Rochais. "Analysis of skeletal diversity of multi-target directed ligands (MTDLs) targeting Alzheimer's disease." European Journal of Medicinal Chemistry 286 (March 2025): 117277. https://doi.org/10.1016/j.ejmech.2025.117277.

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Drakontaeidi, Aliki, and Eleni Pontiki. "Multi-Target-Directed Cinnamic Acid Hybrids Targeting Alzheimer’s Disease." International Journal of Molecular Sciences 25, no. 1 (2024): 582. http://dx.doi.org/10.3390/ijms25010582.

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Progressive cognitive decline in Alzheimer’s disease (AD) is a growing challenge. Present therapies are based on acetylcholinesterase inhibition providing only temporary relief. Promising alternatives include butyrylcholinesterase (BuChE) inhibitors, multi-target ligands (MTDLs) that address the multi-factorial nature of AD, and compounds that target oxidative stress and inflammation. Cinnamate derivatives, known for their neuroprotective properties, show potential when combined with established AD agents, demonstrating improved efficacy. They are being positioned as potential AD therapeutic l
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Dissertations / Theses on the topic "Multi-target directed ligands (MTDLs)"

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Simoni, Elena <1979&gt. "Multi-target-directed ligands: application to the Alzheimer's disease." Doctoral thesis, Alma Mater Studiorum - Università di Bologna, 2010. http://amsdottorato.unibo.it/2848/1/elena.simoni_tesi.pdf.pdf.

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The MTDL (multi-target-directed ligand) design strategy is used to develop single chemical entities that are able to simultaneously modulate multiple targets. The development of such compounds might disclose new avenues for the treatment of a variety of pathologies (e.g. cancer, AIDS, neurodegenerative diseases), for which an effective cure is urgently needed. This strategy has been successfully applied to Alzheimer’s disease (AD) due to its multifactorial nature, involving cholinergic dysfunction, amyloid aggregation, and oxidative stress. Despite many biological entities have been recognized
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Simoni, Elena <1979&gt. "Multi-target-directed ligands: application to the Alzheimer's disease." Doctoral thesis, Alma Mater Studiorum - Università di Bologna, 2010. http://amsdottorato.unibo.it/2848/.

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The MTDL (multi-target-directed ligand) design strategy is used to develop single chemical entities that are able to simultaneously modulate multiple targets. The development of such compounds might disclose new avenues for the treatment of a variety of pathologies (e.g. cancer, AIDS, neurodegenerative diseases), for which an effective cure is urgently needed. This strategy has been successfully applied to Alzheimer’s disease (AD) due to its multifactorial nature, involving cholinergic dysfunction, amyloid aggregation, and oxidative stress. Despite many biological entities have been recognized
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Pérez, Areales Francisco Javier. "Novel multi-target directed ligands as drug candidates against Alzheimer’s disease." Doctoral thesis, Universitat de Barcelona, 2017. http://hdl.handle.net/10803/404781.

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Alzheimer’s disease (AD) is the main neurodegenerative disorder and one of the most important health-care problems worldwide, because of its high prevalence and personal and economic impact. To aggravate this situation, current treatments are only symptomatic, but do not prevent, halt, or delay the disease progression. In the light of the multiple mechanisms involved in its pathogenesis, such as dysfunction of cholinergic and glutamatergic neurotransmitter systems, amyloid and tau pathologies, or oxidative stress, among others, the traditional medicinal chemistry approach of developing drugs b
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Milelli, Andrea <1980&gt. "New Synthetic Polyamines as Multi-Target-Directed Ligands for the Treatment of Alzheimer's Disease and Cancer: Design, Synthesis and Biological Evaluation." Doctoral thesis, Alma Mater Studiorum - Università di Bologna, 2009. http://amsdottorato.unibo.it/1763/1/milelli_andrea_tesi.pdf.

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Alzheimer's disease (AD) and cancer represent two of the main causes of death worldwide. They are complex multifactorial diseases and several biochemical targets have been recognized to play a fundamental role in their development. Basing on their complex nature, a promising therapeutical approach could be represented by the so-called "Multi-Target-Directed Ligand" approach. This new strategy is based on the assumption that a single molecule could hit several targets responsible for the onset and/or progression of the pathology. In particular in AD, most currently prescribed drugs aim to incr
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Milelli, Andrea <1980&gt. "New Synthetic Polyamines as Multi-Target-Directed Ligands for the Treatment of Alzheimer's Disease and Cancer: Design, Synthesis and Biological Evaluation." Doctoral thesis, Alma Mater Studiorum - Università di Bologna, 2009. http://amsdottorato.unibo.it/1763/.

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Alzheimer's disease (AD) and cancer represent two of the main causes of death worldwide. They are complex multifactorial diseases and several biochemical targets have been recognized to play a fundamental role in their development. Basing on their complex nature, a promising therapeutical approach could be represented by the so-called "Multi-Target-Directed Ligand" approach. This new strategy is based on the assumption that a single molecule could hit several targets responsible for the onset and/or progression of the pathology. In particular in AD, most currently prescribed drugs aim to incr
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Guiselin, Thomas. "Cοnceptiοn, synthèse et évaluatiοn biοlοgique de ligands sérοtοninergiques multicibles d’intérêt dans la maladie d’Alzheimer". Electronic Thesis or Diss., Normandie, 2024. http://www.theses.fr/2024NORMC221.

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La Maladie d’Alzheimer (MA) est une maladie neurodégénérative multifactorielle et est considérée comme la démence la plus commune, liée à l’âge. Actuellement, les médicaments disponibles en France sont en majorité des inhibiteurs de l’acétylcholinestérase (AChE) qui n’offrent que peu d’effets symptomatiques accompagnés d’effets secondaires importants. En parallèle, le système sérotoninergique, hypothèse supplémentaire d’apparition de la maladie, est une cible potentielle pour le traitement de la MA. Son origine multifactorielle a mené au recours croissant à la stratégie pléiotrope, visant à in
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Lanthier, Caroline. "Conception, synthèse et évaluation de nouveaux composés à dualité d'action agoniste des récepteurs 5-HT4 et antioxydante, d'intérêt thérapeutique pléiotrope dans la maladie d'Alzheimer Novel multi target-directed ligands targeting 5-HT 4 receptors with in cellulo antioxidant properties as promising leads in Alzheimer's disease Novel potent Benzisoxazoles targeting 5-HT4 receptors with in cellulo antioxidant properties as promising leads for Alzheimer disease." Thesis, Normandie, 2020. http://www.theses.fr/2020NORMC415.

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La maladie d’Alzheimer est une maladie neurodégénérative caractérisée par des pertes de mémoire et des troubles cognitifs. Bien qu’à l’heure actuelle, les causes physiopathologiques de la MA ne soient pas entièrement connues, un certain nombre de causes moléculaires ont été identifiées telles que l’agrégation des peptides β-amyloïdes, les dégénérescences neurofibrillaires liées à la protéine Tau, le stress oxydant et les phénomènes de neuroinflammation. Les traitements actuels de la MA sont des traitements symptomatiques tels que les inhibiteurs d’acétylcholinestérase ne permettant pas de trai
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Łozińska, Iwona. "Synteza i badania biologiczne nowych inhibitorów cholinoesteraz zawierających ugrupowanie serotoniny i wybranych pochodnych heterocyklicznych." Doctoral thesis, 2016. https://depotuw.ceon.pl/handle/item/1630.

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Projektowanie nowych inhibitorów cholinoesteraz jest bardzo istotnym elementem poszukiwania leków w chorobie Alzheimera. Wśród obecnie stosowanych farmaceutyków w terapii tej choroby znajduje się m.in. takryna i donepezil, odwracalne inhibitory cholinoesteraz – acetylocholinoesterazy (AChE) oraz butyrylocholinowesterazy (BChE), których pochodne stały się elementami budulcowymi do otrzymania inhibitorów, objętych rozprawą doktorską. Etiologia choroby Alzheimera nie jest jeszcze poznana, natomiast wiadomym jest, iż jest to choroba wieloczynnikowa, w leczeniu której działanie na pojedynczy
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Book chapters on the topic "Multi-target directed ligands (MTDLs)"

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Das, Sucharita, and Soumalee Basu. "Strategies for Multi-Target Directed Ligands: Application in Alzheimer’s Disease (AD) Therapeutics." In Methods in Pharmacology and Toxicology. Springer New York, 2018. http://dx.doi.org/10.1007/7653_2018_8.

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Ortiz, Cindy Juliet Cristancho, Matheus de Freitas Silva, Vanessa Silva Gontijo, Flávia Pereira Dias Viegas, Kris Simone Tranches Dias, and Claudio Viegas. "Design of Multi-target Directed Ligands as a Modern Approach for the Development of Innovative Drug Candidates for Alzheimer’s Disease." In Methods in Pharmacology and Toxicology. Springer New York, 2018. http://dx.doi.org/10.1007/7653_2018_2.

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de Freitas Silva, Matheus, Flávia Pereira Dias Viegas, Vanessa Silva Gontijo, et al. "Multi-functional Ligands and Molecular Hybridization: Conceptual Aspects and Application in the Innovative Design of Drug Candidate Prototypes for Neurodegenerative Diseases." In Frontiers in Clinical Drug Research - CNS and Neurological Disorders. BENTHAM SCIENCE PUBLISHERS, 2023. http://dx.doi.org/10.2174/9789815123319123110003.

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The rapid increase in the incidence of dementia has enormous socio.economic impacts and costs for governmental health systems all over the world. Despite this, finding an effective treatment for the different types of neurodegenerative diseases (NDs) so far represents a challenge for science. The biggest obstacles related to NDs are their multifactorial complexity and the lack of knowledge of the different pathophysiological pathways involved in the development of each disorder. The latest advances in science, especially those related to the systems biology concepts, have given new insights fo
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"The Development of Multi-Target-Directed Ligands (MTDL) to Treat Alzheimer’s Disease." In Frontiers in Clinical Drug Research – Alzheimer Disorders, edited by John W. Wright and Joseph W. Harding. BENTHAM SCIENCE PUBLISHERS, 2013. http://dx.doi.org/10.2174/9781608057221113010004.

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Ambure, Pravin, and Kunal Roy. "Computer-Aided Drug Design for the Identification of Multi-Target Directed Ligands (MTDLs) in Complex Diseases: An Overview." In Pharmaceutical Biocatalysis. Jenny Stanford Publishing, 2019. http://dx.doi.org/10.1201/9780429295034-19.

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Nepovimova, Eugenie, and Kamil Kuca. "Multi-Target-Directed Ligands in Alzheimer’s Disease Therapy." In Neurodegenerative Diseases - Molecular Mechanisms and Current Therapeutic Approaches [Working Title]. IntechOpen, 2020. http://dx.doi.org/10.5772/intechopen.93269.

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Gong Cheng-Xin, Liu Fei, and Iqbal Khalid. "Multifactorial Hypothesis and Multi-Targets for Alzheimer's Disease." In Advances in Alzheimer’s Disease. IOS Press, 2018. https://doi.org/10.3233/978-1-61499-876-1-105.

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The amyloid cascade hypothesis has been dominating drug discovery for Alzheimer's disease (AD) for the last two decades. The failure of the development of effective drugs for slowing down or reversing the progression of AD warrants the AD field to consider out-of-the-box thinking and therapeutic approaches. We propose the multifactorial hypothesis of AD, emphasizing that AD is caused by multiple etiological factors, which may result in common brain pathology and functional consequences through several separate but integrated molecular pathways. More than one etiological factor and mechanistic
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Conference papers on the topic "Multi-target directed ligands (MTDLs)"

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West, Ryan, and Stevan Pecic. "Multi-Target Directed Ligands for the Treatment of Alzheimer’s Disease." In ASPET 2023 Annual Meeting Abstracts. American Society for Pharmacology and Experimental Therapeutics, 2023. http://dx.doi.org/10.1124/jpet.122.183150.

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Tyagi, Ankit, Shikhar Gupta, and C. Gopi Mohan. "In silicoapproach to discover multi-target-directed ligands for the treatment of Alzheimer's disease." In the International Symposium. ACM Press, 2010. http://dx.doi.org/10.1145/1722024.1722032.

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Pecic, Stevan, Jeannes Angelia, and Xiaohui Weng. "Design, Synthesis and Biological Evaluation of Benzothiazole-Phenyl Analogs as Multi-Target Directed Ligands for Treating Pain." In ASPET 2023 Annual Meeting Abstracts. American Society for Pharmacology and Experimental Therapeutics, 2023. http://dx.doi.org/10.1124/jpet.122.143050.

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