Multitarget‐Directed Ligands Combining Cholinesterase and Monoamine Oxidase Inhibition with Histamine H3R Antagonism for Neurodegenerative Diseases

The role of oxidative stress in neurodegenerative diseases

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Oxidative Stress in Neurodegenerative Diseases

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The histamine H3 receptor: from discovery to clinical trials with pitolisant

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Acetylcholinesterase inhibitors: novel activities of old molecules

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Synthesis, Biological Evaluation, and Molecular Modeling of Donepezil and N-[(5-(Benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine Hybrids as New Multipotent Cholinesterase/Monoamine Oxidase Inhibitors for the Treatment of Alzheimer’s Disease

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Keynote review: Histamine H3 receptor antagonists reach out for the clinic

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Tacrine–Melatonin Hybrids as Multifunctional Agents for Alzheimer's Disease, with Cholinergic, Antioxidant, and Neuroprotective Properties

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Histamine H3 receptor as a potential target for cognitive symptoms in neuropsychiatric diseases

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Distinct pharmacology of rat and human histamine H3 receptors: role of two amino acids in the third transmembrane domain

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A perspective on multi‐target drug discovery and design for complex diseases

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Polypharmacology by Design: A Medicinal Chemist’s Perspective on Multitargeting Compounds

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From combinations to multitarget-directed ligands: A continuum in Alzheimer’s disease polypharmacology

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Alzheimer’s Disease, the “One-Molecule, One-Target” Paradigm, and the Multitarget Directed Ligand Approach

Oset‐Gasque, M. J., & Marco‐Contelles, J. (2018) · ACS Chemical Neuroscience · doi:10.1021/acschemneuro.8b00069 · Cited by 160

Polymeric Nanoparticles for Nasal Drug Delivery to the Brain: Relevance to Alzheimer's Disease

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MAO inhibitors and their wider applications: a patent review

Carradori, S., Secci, D., & Petzer, J. P. (2018) · Expert Opinion on Therapeutic Patents · doi:10.1080/13543776.2018.1427735 · Cited by 139

Monoamine oxidase‐B inhibitors as potential neurotherapeutic agents: An overview and update

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Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer’s disease (1998–2018)

Mishra, P., Kumar, A., & Panda, G. (2019) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2019.01.025 · Cited by 130

Alzheimer's disease: Updated multi-targets therapeutics are in clinical and in progress

Sang, Z., Wang, K., Dong, J., & Tang, L. (2022) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2022.114464 · Cited by 127

Kinetics, mechanism, and inhibition of monoamine oxidase

Ramsay, R. R., & Albreht, A. (2018) · Journal of Neural Transmission · doi:10.1007/s00702-018-1861-9 · Cited by 108

Recent advances in dopaminergic strategies for the treatment of Parkinson’s disease

Mao, Q., Qin, W., Zhang, A., & Ye, N. (2020) · Acta Pharmacologica Sinica · doi:10.1038/s41401-020-0365-y · Cited by 92

Small-Molecule Inhibitors of Reactive Oxygen Species Production

Sassetti, E., Clausen, M. H., & Laraia, L. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c01914 · Cited by 85

The current status of pharmacotherapy for the treatment of Parkinson’s disease: transition from single-target to multitarget therapy

Cheong, S. L., Federico, S., Spalluto, G., Klotz, K., & Pastorin, G. (2019) · Drug Discovery Today · doi:10.1016/j.drudis.2019.05.003 · Cited by 76

Histamine H3 receptor antagonists/inverse agonists: Where do they go?

Ghamari, N., Zarei, O., Arias‐Montaño, J., Reiner‐Link, D., Dastmalchi, S., Stark, H., & Hamzeh‐Mivehroud, M. (2019) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2019.04.007 · Cited by 65

Contilisant, a Tetratarget Small Molecule for Alzheimer’s Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile

Bautista‐Aguilera, Ó. M., Budni, J., Mina, F., Medeiros, E. B., Deuther‐Conrad, W., Entrena, J. M., Moraleda, I., Iriepa, I., Lopez-Munoz, F. J., & Marco, J. L. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b00848 · Cited by 64

Novel approaches to the discovery of selective human monoamine oxidase-B inhibitors: is there room for improvement?

Guglielmi, P., Carradori, S., Ammazzalorso, A., & Secci, D. (2019) · Expert Opinion on Drug Discovery · doi:10.1080/17460441.2019.1637415 · Cited by 58

Multi-Target-Directed Ligands as an Effective Strategy for the Treatment of Alzheimer’s Disease

Kumar, R., Kumar, V., Kumar, B., Thakur, A., & Dwivedi, A. R. (2021) · Current Medicinal Chemistry · doi:10.2174/0929867328666210512005508 · Cited by 55

Novel indanone derivatives as MAO B/H3R dual-targeting ligands for treatment of Parkinson’s disease

Affini, A., Hagenow, S., Živković, A., Marco, J. L., & Stark, H. (2018) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2018.02.015 · Cited by 53

Novel multitarget-directed ligands targeting acetylcholinesterase and σ1 receptors as lead compounds for treatment of Alzheimer's disease: Synthesis, evaluation, and structural characterization of their complexes with acetylcholinesterase

Lalut, J., Santoni, G., Karila, D., Lecoutey, C., Davis, A., Nachon, F., Silman, I., Sussman, J. L., Weik, M., Maurice, T., et al. (2018) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2018.10.064 · Cited by 53

Novel benzothiazole derivatives as multitargeted-directed ligands for the treatment of Alzheimer’s disease

Hafez, D. E., Dubiel, M., Spada, G. L., Catto, M., Reiner‐Link, D., Syu, Y.-T., Abdel‐Halim, M., Hwang, T., Stark, H., & Abadi, A. (2023) · Journal of Enzyme Inhibition and Medicinal Chemistry · doi:10.1080/14756366.2023.2175821 · Cited by 50

Structural and Molecular Insight into Piperazine and Piperidine Derivatives as Histamine H3 and Sigma-1 Receptor Antagonists with Promising Antinociceptive Properties

Szczepańska, K., Podlewska, S., Dichiara, M., Gentile, D., Patamia, V., Rosier, N., Mönnich, D., Ruiz‐Cantero, M. C., Karcz, T. P., Łażewska, D., et al. (2021) · ACS Chemical Neuroscience · doi:10.1021/acschemneuro.1c00435 · Cited by 49

Selenazolyl-hydrazones as Novel Selective MAO Inhibitors With Antiproliferative and Antioxidant Activities: Experimental and In-silico Studies

Elshaflu, H., Todorović, T. R., Nikolic, M. R., Lolić, A., Višnjevac, A., Hagenow, S., Padrón, J. M., García‐Sosa, A. T., Đorđević, I., Grubišić, S., et al. (2018) · Frontiers in Chemistry · doi:10.3389/fchem.2018.00247 · Cited by 49

8-Hydroxyquinolylnitrones as multifunctional ligands for the therapy of neurodegenerative diseases

Knez, D., Diez‐Iriepa, D., Chioua, M., Gottinger, A., Denic, M., Chantegreil, F., Nachon, F., Brazzolotto, X., Skrzypczak-Wiercioch, A., Meden, A., et al. (2023) · Acta Pharmaceutica Sinica B · doi:10.1016/j.apsb.2023.01.013 · Cited by 46

Design, Synthesis, and Biological Evaluation of 2-(Benzylamino-2-Hydroxyalkyl)Isoindoline-1,3-Diones Derivatives as Potential Disease-Modifying Multifunctional Anti-Alzheimer Agents

Panek, D., Więckowska, A., Pasieka, A., Godyń, J., Jończyk, J., Bajda, M., Knez, D., Gobec, S., & Malawska, B. (2018) · Molecules · doi:10.3390/molecules23020347 · Cited by 46

New Dual Small Molecules for Alzheimer’s Disease Therapy Combining Histamine H 3 Receptor (H3R) Antagonism and Calcium Channels Blockade with Additional Cholinesterase Inhibition

Malek, R., Arribas, R. L., Palomino-Antolin, A., Totoson, P., Demougeot, C., Kobrlova, T., Soukup, O., Iriepa, I., Moraleda, I., Diez-Iriepa, D., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b00937 · Cited by 45

Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands

Rodríguez‐Soacha, D. A., Scheiner, M., & Decker, M. W. (2019) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2019.07.040 · Cited by 44

Propargylamine-derived multi-target directed ligands for Alzheimer’s disease therapy

Carreiras, M. C., Ismaïli, L., & Marco, J. L. (2019) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2019.126880 · Cited by 45

Enhancing the Therapeutic Effect in Alzheimer's Disease Drugs: The role of Polypharmacology and Cholinesterase inhibitors

Martins, M. M., Branco, P. S., & Ferreira, L. M. (2023) · ChemistrySelect · doi:10.1002/slct.202300461 · Cited by 50

Recent advances in multitarget-directed ligands targeting G-protein-coupled receptors

Ma, H., Huang, B., & Zhang, Y. (2020) · Drug Discovery Today · doi:10.1016/j.drudis.2020.07.004 · Cited by 43

Probing Fluorinated Motifs onto Dual AChE-MAO B Inhibitors: Rational Design, Synthesis, Biological Evaluation, and Early-ADME Studies

Rullo, M., Cipolloni, M., Catto, M., Colliva, C., Miniero, D. V., Latronico, T., de Candia, M., Benicchi, T., Linusson, A., Giacchè, N., et al. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c01784 · Cited by 41

Synthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine H3R ligands

Szczepańska, K., Karcz, T. P., Mogilski, S., Siwek, A., Kuder, K., Latacz, G., Kubacka, M., Hagenow, S., Lubelska, A., Olejarz‐Maciej, A., et al. (2018) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2018.04.043 · Cited by 34

Rational design of new multitarget histamine H3 receptor ligands as potential candidates for treatment of Alzheimer’s disease

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Molecular Modeling of Histamine Receptors—Recent Advances in Drug Discovery

Mehta, P., Miszta, P., & Filipek, S. (2021) · Molecules · doi:10.3390/molecules26061778 · Cited by 34

Progress in the development of histamine H3 receptor antagonists/inverse agonists: a patent review (2013-2017)

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Novel naphthyloxy derivatives – Potent histamine H3 receptor ligands. Synthesis and pharmacological evaluation

Łażewska, D., Kaleta, M., Hagenow, S., Mogilski, S., Latacz, G., Karcz, T. P., Lubelska, A., Honkisz-Orzechowska, E., Handzlik, J., Reiner‐Link, D., et al. (2018) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2018.04.023 · Cited by 29

New tacrine–acridine hybrids as promising multifunctional drugs for potential treatment of Alzheimer's disease

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Parameters for Irreversible Inactivation of Monoamine Oxidase

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Dual Piperidine-Based Histamine H 3 and Sigma-1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain

Szczepańska, K., Karcz, T. P., Dichiara, M., Mogilski, S., Kalinowska‐Tłuścik, J., Pilarski, B., Leniak, A., Pietruś, W., Podlewska, S., Popiołek-Barczyk, K., et al. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c00430 · Cited by 25

Histamine H3 receptor and cholinesterases as synergistic targets for cognitive decline: Strategies to the rational design of multitarget ligands

Lopes, F. B., Aranha, C. M. S. Q., & Fernandes, J. P. S. (2021) · Chemical Biology & Drug Design · doi:10.1111/cbdd.13866 · Cited by 22

Cyanobiphenyls: Novel H3 receptor ligands with cholinesterase and MAO B inhibitory activity as multitarget compounds for potential treatment of Alzheimer’s disease

Godyń, J., Zaręba, P., Łażewska, D., Stary, D., Reiner‐Link, D., Frank, A., Latacz, G., Mogilski, S., Kaleta, M., Doroż-Płonka, A., et al. (2021) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2021.105129 · Cited by 21

Dual Target Ligands with 4-tert-Butylphenoxy Scaffold as Histamine H3 Receptor Antagonists and Monoamine Oxidase B Inhibitors

Łażewska, D., Olejarz‐Maciej, A., Reiner‐Link, D., Kaleta, M., Latacz, G., Zygmunt, M., Doroż-Płonka, A., Karcz, T. P., Frank, A., Stark, H., et al. (2020) · International Journal of Molecular Sciences · doi:10.3390/ijms21103411 · Cited by 21

Multitarget-directed Ligands for Neurodegenerative Diseases: Real Opportunity Or Blurry mirage?

Benchekroun, M., & Maramai, S. (2019) · Future Medicinal Chemistry · doi:10.4155/fmc-2018-0249 · Cited by 21

Synthesis of Chromone‐Containing Allylmorpholines through a Morita–Baylis–Hillman‐Type Reaction

Chernov, N. M., Shutov, R. V., Barygin, O. I., Dron, M. Y., Старова, Г. Л., Kuzmich, N. N., & Yakovlev, I. P. (2018) · European Journal of Organic Chemistry · doi:10.1002/ejoc.201801159 · Cited by 19

Contilisant+Tubastatin A Hybrids: Polyfunctionalized Indole Derivatives as New HDAC Inhibitor-Based Multitarget Small Molecules with In Vitro and In Vivo Activity in Neurodegenerative Diseases

Toledano‐Pinedo, M., Porro-Pérez, A., Schäker‐Hübner, L., Romero, F., Dong, M., Samadi, A., Almendros, P., Iriepa, I., Bautista‐Aguilera, Ó. M., Rodríguez‐Fernández, M. M., et al. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c01367 · Cited by 19

Structural modifications and in vitro pharmacological evaluation of 4-pyridyl-piperazine derivatives as an active and selective histamine H3 receptor ligands

Szczepańska, K., Karcz, T. P., Siwek, A., Kuder, K., Latacz, G., Bednarski, M., Szafarz, M., Hagenow, S., Lubelska, A., Olejarz‐Maciej, A., et al. (2019) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2019.103071 · Cited by 18

4-tert-Pentylphenoxyalkyl derivatives – Histamine H3 receptor ligands and monoamine oxidase B inhibitors

Łażewska, D., Olejarz‐Maciej, A., Kaleta, M., Bajda, M., Siwek, A., Karcz, T. P., Doroż-Płonka, A., Cichoń, U., Kuder, K., & Kieć‐Kononowicz, K. (2018) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2018.10.048 · Cited by 18

The Evolution of AChE Inhibitors in Alzheimer's Disease: From Single‐Target to Multi‐Target Ligands

Mehta, N. V., Kapadia, A., Khambete, M., & Abhyankar, A. N. (2025) · ChemBioChem · doi:10.1002/cbic.202500053 · Cited by 20

An Update of Synthetic Approaches and Structure‐Activity Relationships of Various Classes of Human MAO‐B Inhibitors

Sharma, P., Singh, M., & Mathew, B. (2021) · ChemistrySelect · doi:10.1002/slct.202004188 · Cited by 17

Conceptual Framework of the Design of Pleiotropic Drugs against Alzheimer’s Disease

Guiselin, T., Lecoutey, C., Rochais, C., & Dallemagne, P. (2023) · Pharmaceutics · doi:10.3390/pharmaceutics15102382 · Cited by 16

Adenosine A2AR/A1R Antagonists Enabling Additional H3R Antagonism for the Treatment of Parkinson’s Disease

Hagenow, S., Affini, A., Pioli, E. Y., Hinz, S., Zhao, Y., Porras, G., Namasivayam, V., Müller, C. E., Lin, J., Bézard, E., et al. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00914 · Cited by 15

Rasagiline derivatives combined with histamine H3 receptor properties

Lutsenko, K., Hagenow, S., Affini, A., Reiner‐Link, D., & Stark, H. (2019) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2019.08.016 · Cited by 15

Discovery of novel multifunctional ligands targeting GABA transporters, butyrylcholinesterase, β-secretase, and amyloid β aggregation as potential treatment of Alzheimer's disease

Zaręba, P., Łątka, K., Mazur, G., Gryzło, B., Pasieka, A., Godyń, J., Panek, D., Skrzypczak-Wiercioch, A., Höfner, G. C., Latacz, G., et al. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.115832 · Cited by 15

In silico and in vitro studies of two non‐imidazole multiple targeting agents at histamine H3 receptors and cholinesterase enzymes

Ghamari, N., Dastmalchi, S., Zarei, O., Arias‐Montaño, J., Reiner‐Link, D., Alkan, F. Ü., Stark, H., & Hamzeh‐Mivehroud, M. (2019) · Chemical Biology & Drug Design · doi:10.1111/cbdd.13642 · Cited by 14

In Vitro and In Silico ADME-Tox Profiling and Safety Significance of Multifunctional Monoamine Oxidase Inhibitors Targeting Neurodegenerative Diseases

Więckowska, A., Szałaj, N., Góral, I., Bucki, A., Latacz, G., Kieć‐Kononowicz, K., Bautista‐Aguilera, Ó. M., Romero, A., Ramos, E., Egea, J., et al. (2020) · ACS Chemical Neuroscience · doi:10.1021/acschemneuro.0c00489 · Cited by 14

Design, synthesis and biological evaluation of 2-styryl-5-hydroxy-4-pyrone derivatives and analogues as multiple functional agents with the potential for the treatment of Alzheimer's disease.

Hu, C., Jiang, L., Tang, L., Zhang, M.-K., & Sheng, R. (2021) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2021.116306 · Cited by 11

Questions in the Chemical Enzymology of MAO

Ramsay, R. R., & Albreht, A. (2021) · Chemistry · doi:10.3390/chemistry3030069 · Cited by 13

Design, Synthesis, and In Vitro Biological Activities of a Bio-Oxidizable Prodrug to Deliver Both ChEs and DYRK1A Inhibitors for AD Therapy

Barré, A., Azzouz, R., Gembus, V., Papamicaël, C. A., & Levacher, V. (2019) · Molecules · doi:10.3390/molecules24071264 · Cited by 12

Epigenetics meets GPCR: inhibition of histone H3 methyltransferase (G9a) and histamine H3 receptor for Prader–Willi Syndrome

Reiner‐Link, D., Seifert, L., Deck, C., Schüle, R., Jung, M., & Stark, H. (2020) · Scientific Reports · doi:10.1038/s41598-020-70523-y · Cited by 12

Privileged multi-target directed propargyl-tacrines combining cholinesterase and monoamine oxidase inhibition activities

Chrienová, Ž., Nepovimová, E., Andrýs, R., Doležal, R., Janočková, J., Múčková, Ľ., Fabova, L., Soukup, O., Olekšák, P., Vališ, M., et al. (2022) · Journal of Enzyme Inhibition and Medicinal Chemistry · doi:10.1080/14756366.2022.2122054 · Cited by 11

Calcium channel blockers’ contribution to overcoming Current drug discovery challenges in Alzheimer’s disease

Bernard, P. J., Bellili, D., & Ismaïli, L. (2023) · Expert Opinion on Drug Discovery · doi:10.1080/17460441.2023.2266994 · Cited by 12

Prior Activation of 5-HT7 Receptors Modulates the Conditioned Place Preference With Methylphenidate

Carbone, C., Russo, S. L. M. L., Lacivita, E., Frank, A., Alleva, E., Stark, H., Saso, L., Leopoldo, M., & Adriani, W. (2019) · Frontiers in Behavioral Neuroscience · doi:10.3389/fnbeh.2019.00208 · Cited by 11

Histamine H3 receptor antagonists with peptidomimetic (keto)piperazine structures to inhibit Aβ oligomerisation

Falkenstein, M., Reiner‐Link, D., Živković, A., Gering, I., Willbold, D., & Stark, H. (2021) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2021.116462 · Cited by 12

The Chemotype of Chromanones as a Privileged Scaffold for Multineurotarget Anti-Alzheimer Agents

Keuler, T., Lemke, C., Elsinghorst, P. W., Iriepa, I., Chioua, M., MARTINEZ‐GRAU, A., Beadle, C. D., Vetman, T. N., Lopez-Munoz, F. J., Wille, T., et al. (2022) · ACS Pharmacology & Translational Science · doi:10.1021/acsptsci.2c00097 · Cited by 10

Polyfunctionalized α-Phenyl-tert-butyl(benzyl)nitrones: Multifunctional Antioxidants for Stroke Treatment

Diez‐Iriepa, D., Knez, D., Gobec, S., Iriepa, I., Rı́os, C. D. L., Bravo, I., Lopez-Munoz, F. J., Marco‐Contelles, J., & Hadjipavlou‐Litina, D. (2022) · Antioxidants · doi:10.3390/antiox11091735 · Cited by 10

Dual-targeting Approach on Histamine H3 and Sigma-1 Receptor Ligands as Promising Pharmacological Tools in the Treatment of CNS-linked Disorders

Szczepańska, K., Kuder, K., & Kieć‐Kononowicz, K. (2020) · Current Medicinal Chemistry · doi:10.2174/0929867327666200806103144 · Cited by 10

The Novel Pimavanserin Derivative ST-2300 with Histamine H3 Receptor Affinity Shows Reduced 5-HT2A Binding, but Maintains Antidepressant- and Anxiolytic-like Properties in Mice

Venkatachalam, K., Zhong, S., Dubiel, M., Satała, G., Sadek, B. S., & Stark, H. (2022) · Biomolecules · doi:10.3390/biom12050683 · Cited by 9

Scutellarein derivatives with histamine H3 receptor antagonism and cholinesterase inhibitory potency as multi target-directed ligands for possible Alzheimer’s disease therapy

Chen, J., Zhu, H., Luo, K., Luo, Q., Wang, Y., Liu, T., Li, L., Dai, Z., Yang, S., Li, Y., et al. (2024) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2024.107704 · Cited by 8

Design and Synthesis of Arylpiperazine Serotonergic/Dopaminergic Ligands with Neuroprotective Properties

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Repurposing of 8‐Hydroxyquinoline‐Based Butyrylcholinesterase and Cathepsin B Ligands as Potent Nonpeptidic Deoxyribonuclease I Inhibitors

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