Novel Multitarget-Directed Ligands (MTDLs) with Acetylcholinesterase (AChE) Inhibitory and Serotonergic Subtype 4 Receptor (5-HT4R) Agonist Activities As Potential Agents against Alzheimer’s Disease: The Design of Donecopride
Open accessAbstract
In this work, we describe the synthesis and in vitro evaluation of a novel series of multitarget-directed ligands (MTDL) displaying both nanomolar dual-binding site (DBS) acetylcholinesterase inhibitory effects and partial 5-HT4R agonist activity, among which donecopride was selected for further in vivo evaluations in mice. The latter displayed procognitive and antiamnesic effects and enhanced sAPPα release, accounting for a potential symptomatic and disease-modifying therapeutic benefit in the treatment of Alzheimer's disease.
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Co-administration of RS67333 (26) at 0.1 mg/kg and donepezil (1) at 0.3 mg/kg at subactive doses resulted in improved memory performances in mice.
“In this case, 26 (0.1 mg/kg) and 1 (0.3 mg/kg), when co-administrated at subactive doses, resulted in improved memory performances in mice.”
From From combinations to multitarget-directed ligands: A continuum in Alzheimer’s disease polypharmacology (2021) · cites this paper as [108]
Cites
PROTEIN MEASUREMENT WITH THE FOLIN PHENOL REAGENT
Lowry, O. H., Rosebrough, N., Farr, A. L., & Randall, R. (1951) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(19)52451-6 · Cited by 315,771 · see citing works
Sheldrick, G. M. (2007) · Acta Crystallographica Section A Foundations of Crystallography · doi:10.1107/s0108767307043930 · Cited by 87,861 · see citing works
A new and rapid colorimetric determination of acetylcholinesterase activity
Ellman, G. L., Courtney, K. D., Andres, V., & Featherstone, R. M. (1961) · Biochemical Pharmacology · doi:10.1016/0006-2952(61)90145-9 · Cited by 27,221 · see citing works
Development and validation of a genetic algorithm for flexible docking 1 1Edited by F. E. Cohen
Jones, G., Willett, P., Glen, R. C., Leach, A. R., & Taylor, R. (1997) · Journal of Molecular Biology · doi:10.1006/jmbi.1996.0897 · Cited by 6,763 · see citing works
Can the pharmaceutical industry reduce attrition rates?
Kola, I., & Landis, J. (2004) · Nature Reviews Drug Discovery · doi:10.1038/nrd1470 · Cited by 4,167 · see citing works
High-Resolution Crystal Structure of an Engineered Human β 2 -Adrenergic G Protein–Coupled Receptor
Cherezov, V., Rosenbaum, D. M., Hanson, M. A., Rasmussen, S. G. F., Thian, F. S., Kobilka, T. S., Choi, H., Kühn, P., Weis, W. I., Kobilka, B. K., et al. (2007) · Science · doi:10.1126/science.1150577 · Cited by 3,280 · see citing works
Very fast empirical prediction and rationalization of protein pK a values
Li, H., Robertson, A. D., & Jensen, J. H. (2005) · Proteins Structure Function and Bioinformatics · doi:10.1002/prot.20660 · Cited by 2,058 · see citing works
Molecular recognition of receptor sites using a genetic algorithm with a description of desolvation
Jones, G., Willett, P., & Glen, R. C. (1995) · Journal of Molecular Biology · doi:10.1016/s0022-2836(95)80037-9 · Cited by 1,548 · see citing works
An english translation of alzheimer’s 1907 paper, “über eine eigenartige erkankung der hirnrinde”
Stelzmann, R. A., Norman Schnitzlein, H., & Reed Murtagh, F. (1995) · Clinical Anatomy · doi:10.1002/ca.980080612 · Cited by 1,455 · see citing works
Structures of Human Acetylcholinesterase in Complex with Pharmacologically Important Ligands
Cheung, J., Rudolph, M. J., Burshteyn, F., Cassidy, M. S., Gary, E. N., Love, J. D., Franklin, M. C., & Height, J. J. (2012) · Journal of Medicinal Chemistry · doi:10.1021/jm300871x · Cited by 1,377 · see citing works
Designed Multiple Ligands. An Emerging Drug Discovery Paradigm
Morphy, R., & Ranković, Z. (2005) · Journal of Medicinal Chemistry · doi:10.1021/jm058225d · Cited by 1,237 · see citing works
Multi-target-Directed Ligands To Combat Neurodegenerative Diseases
Cavalli, A., Bolognesi, M. L., Minarini, A., Rosini, M., Tumiatti, V., Recanatini, M., & Melchiorre, C. (2008) · Journal of Medicinal Chemistry · doi:10.1021/jm7009364 · Cited by 1,152 · see citing works
Alzheimer's disease: strategies for disease modification
Citron, M. (2010) · Nature Reviews Drug Discovery · doi:10.1038/nrd2896 · Cited by 1,060 · see citing works
Hybrid Molecules with a Dual Mode of Action: Dream or Reality?
Meunier, B. (2007) · Accounts of Chemical Research · doi:10.1021/ar7000843 · Cited by 942 · see citing works
From magic bullets to designed multiple ligands
Morphy, R., Kay, C., & Ranković, Z. (2004) · Drug Discovery Today · doi:10.1016/s1359-6446(04)03163-0 · Cited by 731 · see citing works
World Alzheimer Report 2010: The global economic impact of dementia
Wimo, A. B., & Prince, M. J. (2010) · Cited by 559 · see citing works
beta-Amyloid aggregation induced by human acetylcholinesterase: inhibition studies.
Bartolini, M., Bertucci, C., Cavrini, V., & Andrisano, V. (2003) · Biochemical Pharmacology · doi:10.1016/s0006-2952(02)01514-9 · Cited by 523 · see citing works
Leon, R. M., Garcı́a, A. G., & Marco, J. L. (2011) · Medicinal Research Reviews · doi:10.1002/med.20248 · Cited by 442 · see citing works
Development of a radioligand binding assay for 5‐HT4 receptors in guinea‐pig and rat brain
Grossman, C. J., Kilpatrick, G. J., & Bunce, K. T. (1993) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.1993.tb13617.x · Cited by 290 · see citing works
Lipoic acid as a novel treatment for Alzheimer's disease and related dementias
Holmquist, L., Stuchbury, G., Berbaum, K., Muscat, S., Young, S. A., Häger, K., Engel, J., & Münch, G. W. (2006) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2006.07.001 · Cited by 286 · see citing works
A Technique for Serial Collection of Cerebrospinal Fluid from the Cisterna Magna in Mouse
Liu, L., & Duff, K. (2008) · Journal of Visualized Experiments · doi:10.3791/960 · Cited by 268 · see citing works
Piazzi, L., Rampa, A., Bisi, A., Gobbi, S., Belluti, F., Cavalli, A., Bartolini, M., Andrisano, V., Valenti, P., & Recanatini, M. (2003) · Journal of Medicinal Chemistry · doi:10.1021/jm0340602 · Cited by 268 · see citing works
Designing Multiple Ligands – Medicinal Chemistry Strategies and Challenges
Morphy, R., & Ranković, Z. (2009) · Current Pharmaceutical Design · doi:10.2174/138161209787315594 · Cited by 262 · see citing works
Bolognesi, M. L., Cavalli, A., Valgimigli, L., Bartolini, M., Rosini, M., Andrisano, V., Recanatini, M., & Melchiorre, C. (2007) · Journal of Medicinal Chemistry · doi:10.1021/jm701225u · Cited by 262 · see citing works
Alzheimer disease: progress or profit?
Mount, C., & Downton, C. (2006) · Nature Medicine · doi:10.1038/nm0706-780 · Cited by 262 · see citing works
Multi-Target Drugs: The Trend of Drug Research and Development
Lu, J., Pan, W., Yuanjia, H., & Wang, Y. (2012) · PLoS ONE · doi:10.1371/journal.pone.0040262 · Cited by 259 · see citing works
STERLING, J. J., Herzig, Y., Goren, T., Finkelstein, N., Lerner, D., Goldenberg, W., MISKOLCZI, I., Molnar, S., Rantal, F., Tamás, T., et al. (2002) · Journal of Medicinal Chemistry · doi:10.1021/jm020120c · Cited by 249 · see citing works
The Multifactorial Nature of Alzheimer's Disease for Developing Potential Therapeutics
Carreiras, M. C., Mendes, E., Perry, M. D. J., Francisco, A., & Marco‐Contelles, J. (2013) · Current Topics in Medicinal Chemistry · doi:10.2174/15680266113139990135 · Cited by 242 · see citing works
Multi-Target-Directed Ligands in Alzheimer's Disease Treatment
Bajda, M., Guzior, N., Ignasik, M., & Malawska, B. (2011) · Current Medicinal Chemistry · doi:10.2174/092986711797535245 · Cited by 240 · see citing works
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 · Cited by 225 · see citing works
Muñoz-Ruiz, P., Rubio, L., García‐Palomero, E., Dorronsoro, I., del Monte-Millán, M., Valenzuela, R., Usán, P., de Austria, C., Bartolini, M., Andrisano, V., et al. (2005) · Journal of Medicinal Chemistry · doi:10.1021/jm0503289 · Cited by 221 · see citing works
Therapies for Alzheimer's disease
Melnikova, I. (2007) · Nature Reviews Drug Discovery · doi:10.1038/nrd2314 · Cited by 219 · see citing works
Bockaert, J., Claeysen, S., Compan, V., & Dumuis, A. (2004) · CNS & Neurological Disorders - Drug Targets · doi:10.2174/1568007043482615 · Cited by 207 · see citing works
Self-citationFragments, network biology and designing multiple ligands
Morphy, R., & Ranković, Z. (2006) · Drug Discovery Today · doi:10.1016/j.drudis.2006.12.006 · Cited by 204 · see citing works
Agis-Torres, A., Sollhuber, M., Fernandez, M., & Sanchez-Montero, J. M. (2014) · Current Neuropharmacology · doi:10.2174/1570159x113116660047 · Cited by 202 · see citing works
The Physicochemical Challenges of Designing Multiple Ligands
Morphy, R., & Ranković, Z. (2006) · Journal of Medicinal Chemistry · doi:10.1021/jm0603015 · Cited by 194 · see citing works
Rosini, M., Simoni, E., Bartolini, M., Cavalli, A., Ceccarini, L., Pascu, N., McClymont, D. W., Tarozzi, A., Bolognesi, M. L., Minarini, A., et al. (2008) · Journal of Medicinal Chemistry · doi:10.1021/jm800577j · Cited by 186 · see citing works
Combination Therapy in Alzheimer???s Disease: A Review of Current Evidence
Schmitt, B., Bernhardt, T., Moeller, H.-J., Heuser, I., & Fr??lich, L. (2004) · CNS Drugs · doi:10.2165/00023210-200418130-00001 · Cited by 182 · see citing works
A Small Molecule Targeting the Multifactorial Nature of Alzheimer's Disease
Cavalli, A., Bolognesi, M. L., Capsoni, S., Andrisano, V., Bartolini, M., Margotti, E., Cattaneo, A., Recanatini, M., & Melchiorre, C. (2007) · Angewandte Chemie International Edition · doi:10.1002/anie.200700256 · Cited by 180 · see citing works
How to design multi-target drugs
Korcsmaros, T. D., Szalay, M., Böde, C., Kovács, I. A., & Csermely, P. (2007) · Expert Opinion on Drug Discovery · doi:10.1517/17460441.2.6.799 · Cited by 162 · see citing works
Bolea, I., Gella, A., & Unzeta, M. (2012) · Journal of Neural Transmission · doi:10.1007/s00702-012-0948-y · Cited by 158 · see citing works
The benefits of the multi-target approach in drug design and discovery
Espinoza-Fonseca, M. (2005) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2005.09.011 · Cited by 142 · see citing works
One‐compound‐multiple‐targets strategy to combat Alzheimer's disease
Zhang, H. (2005) · FEBS Letters · doi:10.1016/j.febslet.2005.09.006 · Cited by 139 · see citing works
Lecoutey, C., Hédou, D., Fréret, T., Giannoni, P., Gaven, F., Since, M., Bouët, V., Ballandonne, C., Corvaisier, S., Malzert‐Fréon, A., et al. (2014) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1410315111 · Cited by 136 · see citing works
Self-citationBolognesi, M. L., Andrisano, V., Bartolini, M., Banzi, R., & Melchiorre, C. (2004) · Journal of Medicinal Chemistry · doi:10.1021/jm049156q · Cited by 136 · see citing works
Bolognesi, M. L., Banzi, R., Bartolini, M., Cavalli, A., Tarozzi, A., Andrisano, V., Minarini, A., Rosini, M., Tumiatti, V., Bergamini, C., et al. (2007) · Journal of Medicinal Chemistry · doi:10.1021/jm070559a · Cited by 134 · see citing works
Bolognesi, M. L., Cavalli, A., & Melchiorre, C. (2008) · Neurotherapeutics · doi:10.1016/j.nurt.2008.10.042 · Cited by 117 · see citing works
Marco, J. L., Leon, R. M., Rı́os, C. D. L., Guglietta, A., Terencio, J. V., López, M. G., Garcı́a, A. G., & Villarroya, M. (2006) · Journal of Medicinal Chemistry · doi:10.1021/jm061047j · Cited by 116 · see citing works
Giannoni, P., Gaven, F., Bundel, D. D., Baranger, K., Marchetti, E., Roman, F. S., Valjent, E., Marin, P., Bockaert, J., Rivera, S., et al. (2013) · Frontiers in Aging Neuroscience · doi:10.3389/fnagi.2013.00096 · Cited by 108 · see citing works
Self-citationEglen, R. M., Bonhaus, D. W., Johnson, L. G., Leung, E., & Clark, R. D. (1995) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.1995.tb16628.x · Cited by 102 · see citing works
Dubost⧫, E., Dumas, N., Fossey, C., Magnelli, R., Butt‐Gueulle, S., Ballandonne, C., Caignard, D. H., Dulin, F., Santos, J. S. O., Millet, P., et al. (2012) · Journal of Medicinal Chemistry · doi:10.1021/jm300943r · Cited by 101 · see citing works
Self-citation(2012) · Royal Society of Chemistry eBooks · doi:10.1039/9781849734912 · Cited by 96 · see citing works
Rosini, M., Simoni, E., Minarini, A., & Melchiorre, C. (2014) · Neurochemical Research · doi:10.1007/s11064-014-1250-1 · Cited by 94 · see citing works
Mao, F., Yan, J., Li, J., Jia, X., Miao, H., Sun, Y., Huang, L., & Li, X. (2014) · Organic & Biomolecular Chemistry · doi:10.1039/c4ob00998c · Cited by 91 · see citing works
Pisani, L., Catto, M., Leonetti, F., Nicolotti, O., Stefanachi, A., Campagna, F., & Carotti, A. (2011) · Current Medicinal Chemistry · doi:10.2174/092986711797379302 · Cited by 90 · see citing works
Minarini, A., Milelli, A., Tumiatti, V., Rosini, M., Simoni, E., Bolognesi, M. L., Andrisano, V., Bartolini, M., Motori, E., Angeloni, C., et al. (2011) · Neuropharmacology · doi:10.1016/j.neuropharm.2011.10.007 · Cited by 85 · see citing works
Youdim, M. B. H. (2006) · Current Alzheimer Research · doi:10.2174/156720506779025288 · Cited by 84 · see citing works
Melchiorre, C., Andrisano, V., Bolognesi, M. L., Budriesi, R., Cavalli, A., Cavrini, V., Rosini, M., Tumiatti, V., & Recanatini, M. (1998) · Journal of Medicinal Chemistry · doi:10.1021/jm9810452 · Cited by 81 · see citing works
MTDL Design Strategy in the Context of Alzheimers Disease: From Lipocrine to Memoquin and Beyond
Bolognesi, M. L., Rosini, M., Andrisano, V., Bartolini, M., Minarini, A., Tumiatti, V., & Melchiorre, C. (2009) · Current Pharmaceutical Design · doi:10.2174/138161209787315585 · Cited by 79 · see citing works
Prati, F., Uliassi, E., & Bolognesi, M. L. (2014) · MedChemComm · doi:10.1039/c4md00069b · Cited by 77 · see citing works
Huang, W., Tang, L., Shi, Y., Huang, S., Xu, L., Sheng, R., Wu, P., Li, J. X., Zhou, N., & Hu, Y. (2011) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2011.09.061 · Cited by 75 · see citing works
Enhanced neuronal plasticity and elevated endogenous sAPPα levels in mice over‐expressing MMP9
Fragkouli, A., Papatheodoropoulos, C., Georgopoulos, S., Stamatakis, A., Stylianopoulou, F., Tsilibary, E. C., & Tzinia, A. K. (2011) · Journal of Neurochemistry · doi:10.1111/j.1471-4159.2011.07637.x · Cited by 64 · see citing works
Effects of purine analogues on spontaneous alternation in mice
Hooper, N. K., Fraser, C. M., & Stone, T. W. (1996) · Psychopharmacology · doi:10.1007/bf02246579 · Cited by 64 · see citing works
Bolognesi, M. L., Minarini, A., Rosini, M., et al. (2008) · Mini-Reviews in Medicinal Chemistry · doi:10.2174/138955708785740652 · Cited by 64 · see citing works
Geldenhuys, W. J., & der Schyf, C. J. V. (2012) · Expert Opinion on Drug Discovery · doi:10.1517/17460441.2013.744746 · Cited by 59 · see citing works
Melchiorre, C., Bolognesi, M. L., Minarini, A., Rosini, M., & Tumiatti, V. (2010) · Journal of Medicinal Chemistry · doi:10.1021/jm100293f · Cited by 57 · see citing works
Fréret, T., Bouët, V., Quiedeville, A., Née, G., Dallemagne, P., Rochais, C., & Boulouard, M. (2012) · Behavioural Brain Research · doi:10.1016/j.bbr.2012.02.012 · Cited by 55 · see citing works
Self-citationThe Deacylation Step of Acetylcholinesterase: Computer Simulation Studies
Vagedes, P., Rabenstein, B., Åqvist, J., Marelius, J., & Knapp, E. (2000) · Journal of the American Chemical Society · doi:10.1021/ja0004581 · Cited by 55 · see citing works
Rosenberry, T. L., Mallender, W. D., Thomas, P. J., et al. (1999) · Chemico-Biological Interactions · doi:10.1016/s0009-2797(99)00017-4 · Cited by 55 · see citing works
Chronic 5-HT4 receptor activation decreases Aβ production and deposition in hAPP/PS1 mice.
Tesseur, I., Pimenova, A. A., Lo, A. C., Ciesielska, M., Lichtenthaler, S., Maeyer, J. D. D., Schuurkes, J., D'Hooge, R., & de Strooper, B. (2013) · Neurobiology of Aging · doi:10.1016/j.neurobiolaging.2013.01.020 · Cited by 53 · see citing works
Li, Y., Peng, P., Tang, L., Hu, Y., Hu, Y., & Sheng, R. (2014) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2014.07.009 · Cited by 52 · see citing works
Youdim, M. B. H., Amit, T., Bar‐Am, O., Weinreb, O., & Yogev-Falach, M. (2006) · Neurotoxicity Research · doi:10.1007/bf03033355 · Cited by 46 · see citing works
Brodney, M. A., Johnson, D. E., Sawant‐Basak, A., et al. (2012) · Journal of Medicinal Chemistry · doi:10.1021/jm300953p · Cited by 46 · see citing works
Lipoic Acid, a Lead Structure for Multi-Target-Directed Drugs for Neurodegeneration
Bolognesi, M. L., Minarini, A., Tumiatti, V., & Melchiorre, C. (2006) · Mini-Reviews in Medicinal Chemistry · doi:10.2174/138955706778742731 · Cited by 44 · see citing works
Aguila, B., Coulbault, L., Boulouard, M., Lιveillι, F., Davis, A., Tσth, G., Borsodi, A. D., Balboni, G., Salvadori, S., Jauzac, P., et al. (2007) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0707497 · Cited by 39 · see citing works
Self-citationBartolini, M., Pistolozzi, M., Andrisano, V., Egea, J., López, M. G., Iriepa, I., Moraleda, I., Galvez‐Ruano, E., Marco, J. L., & Samadi, A. (2011) · ChemMedChem · doi:10.1002/cmdc.201100239 · Cited by 26 · see citing works
der Schyf, C. J. V., Geldenhuys, W. J., & Youdim, M. B. H. (2006) · Drugs of the Future · doi:10.1358/dof.2006.031.05.985904 · Cited by 24 · see citing works
Liu, T., Xia, Z., Zhang, W., Xu, J., Ge, X.-X., Li, J., Cui, Y., Qiu, Z., Xu, J., Xie, Q., et al. (2012) · Pharmacology Biochemistry and Behavior · doi:10.1016/j.pbb.2012.11.009 · Cited by 24 · see citing works
Clark, R. D., Jahangir, A. M., Langston, J., et al. (1994) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/s0960-894x(01)80413-3 · Cited by 20 · see citing works
Synthesis of dual AChE/5-HT4 receptor multi-target directed ligands
Lecoutey, C., Rochais, C., Genest, D., Butt‐Gueulle, S., Ballandonne, C., Corvaisier, S., Dulin, F., Lepailleur, A., Santos, J. S. O., & Dallemagne, P. (2012) · MedChemComm · doi:10.1039/c2md20063e · Cited by 18 · see citing works
Self-citationProgress in acetylcholinesterase inhibitors for Alzheimer’s disease
Bolognesi, M. L., Minarini, A., Tumiatti, V., & Melchiorre, C. (2006) · Expert Opinion on Therapeutic Patents · doi:10.1517/13543776.16.6.811 · Cited by 17 · see citing works
A comparison of the pharmacological properties of guinea‐pig and human recombinant 5‐HT4receptors
Vickery, R., Mai, N., Kaufman, E., et al. (2007) · British Journal of Pharmacology · doi:10.1038/sj.bjp.0707154 · Cited by 14 · see citing works
Morphy, R., & Ranković, Z. (2008) · Elsevier eBooks · doi:10.1016/b978-0-12-374194-3.00027-5 · Cited by 12 · see citing works
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Albertini, C., Salerno, A., de Sena Murteira Pinheiro, P., & Bolognesi, M. L. (2021) · Medicinal Research Reviews · doi:10.1002/med.21699 · Cited by 179 · see citing works
Multitarget Therapeutic Strategies for Alzheimer’s Disease: Review on Emerging Target Combinations
Maramai, S., Benchekroun, M., Gabr, M. T., & Yahiaoui, S. (2020) · BioMed Research International · doi:10.1155/2020/5120230 · Cited by 121 · see citing works
Self-citationIn silico repurposing of antipsychotic drugs for Alzheimer’s disease
Kumar, S., Chowdhury, S., & Kumar, S. (2017) · BMC Neuroscience · doi:10.1186/s12868-017-0394-8 · Cited by 103 · see citing works
Uddin, M. S., Al Mamun, A., Kabir, M. T., Ashraf, G. M., Bin-Jumah, M. N., & Abdel-Daim, M. M. (2021) · Molecular Neurobiology · doi:10.1007/s12035-020-02116-9 · Cited by 86 · see citing works
Hu, J., Pan, T., An, B., Li, Z., Li, X., & Huang, L. (2019) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2018.12.013 · Cited by 53 · see citing works
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Mechanistic Insights for Drug Repurposing and the Design of Hybrid Drugs for Alzheimer’s Disease
Padhi, D., & Govindaraju, T. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c00335 · Cited by 47 · see citing works
- Authors
- Rochais, C., Lecoutey, C., Gaven, F., Giannoni, P., Hamidouche, K., Hedou, D., Dubost, E., Genest, D., Yahiaoui, S., Freret, T., Bouet, V., Dauphin, F., Sopkova de Oliveira Santos, J., Ballandonne, C., Corvaisier, S., Malzert-Fréon, A., Legay, R., Boulouard, M., Claeysen, S., & Dallemagne, P.
- Affiliations
- Centre d'Etudes et de Recherche sur le Médicament de Normandie (FR)
- Centre National de la Recherche Scientifique (FR)
- Université de Caen Normandie (FR)
- UNICAEN, CERMN (Centre d’Etudes et de Recherche sur le Médicament de Normandie), F-14032 Caen, France
- UNICAEN, GMPc5 (Groupe Mémoire et Plasticité comportementale), F-14032 Caen, France
- Corresponding author
- Rochais, Christophe
- Dallemagne, Patrick
- ORCID
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2015-03-31
- Volume
- 58
- Issue
- 7
- Pages
- 3172-3187
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2333346687
- Cited by
- 129
- References
- 83
- Citations by year
- 2026: 7 · 2025: 7 · 2024: 10 · 2023: 8 · 2022: 5 · 2021: 13 · 2020: 20 · 2019: 17 · 2018: 14 · 2017: 11 · 2016: 14 · 2015: 3
- FWCI
- 10.34
- Type
- journal article
- Language
- en
- Open access
- green
- hal.science
- Licence
- other-oa
- Locations
- Journal of Medicinal Chemistry (publishedVersion)
- PubMed (publishedVersion)
- HAL (submittedVersion, other-oa)
- Funders
- Agence Nationale de la Recherche (ANR-12-BSV4-008-01, ANR-12-JS007-0012-01)
- Conseil Régional de Basse-Normandie
- Ligue Européenne Contre la Maladie d'Alzheimer (12721)
- Topics
- Health Sciences › Medicine › Pharmacology › Cholinesterase and Neurodegenerative Diseases
- Health Sciences › Medicine › Physiology › Alzheimer's disease research and treatments
- Physical Sciences › Chemistry › Organic Chemistry › Synthesis and biological activity
- Keywords
- multi-target-directed ligands, acetylcholinesterase inhibition, Alzheimer's disease, dual binding sites, procognitive effects, anti-amnesic effect, disease-modifying therapy, drug design
- MeSH terms
- Alzheimer Disease, Aniline Compounds, Animals, Cholinesterase Inhibitors, Computer Simulation, Drug Evaluation, Preclinical, Guinea Pigs, Humans, Ligands, Male, Memory, Short-Term, Mice, Inbred C57BL, Mice, Inbred Strains, Piperidines, Structure-Activity Relationship, Drug Design, Crystallography, X-Ray, Toxicity Tests, Acute, Receptors, Serotonin, 5-HT4, Serotonin 5-HT4 Receptor Agonists, Molecular Targeted Therapy
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
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