ArticleAngewandte Chemie (International ed. in English)2025
Multifunctional, Fluorene-Based Modulator of Cholinergic and GABAergic Neurotransmission as a Novel Drug Candidate for Palliative Treatment of Alzheimer's Disease.
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Article in Angewandte Chemie (International ed. in English), 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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5citing papers in PubMed
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Who cites it
5 citing papers in PubMed.
- Advances in Targeting Central Cholinergic Dysfunction for Neurodegenerative Diseases: From Pharmacotherapy to Neuromodulation.CNS neuroscience & therapeutics · 2026Review
- Evolution of Multitarget Strategies for Alzheimer's Disease: From Cholinergic Inhibition to Network-Oriented Therapeutic Design (2006-2025).Pharmaceuticals (Basel, Switzerland) · 2026Article
- Glial Cells in Behavioral and Psychological Symptoms of Alzheimer's Disease.International journal of molecular sciences · 2026Review
- Alcohol addiction and Alzheimer's disease: a molecular collision course.Translational psychiatry · 2025Review
- Multifunctional, Fluorene-Based Modulator of Cholinergic and GABAergic Neurotransmission as a Novel Drug Candidate for Palliative Treatment of Alzheimer's Disease.Angewandte Chemie (International ed. in English) · 2025Article
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Authors and funding
32 authors.
Dawid PanekDepartment of Physicochemical Drug Analysis, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna St. 9, 30-688, Cracow, Poland.ORCID https://orcid.org/0000-0002-3211-7188
Anna PasiekaDepartment of Physicochemical Drug Analysis, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna St. 9, 30-688, Cracow, Poland.ORCID https://orcid.org/0000-0002-5426-9123
Jakub JończykDepartment of Physicochemical Drug Analysis, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna St. 9, 30-688, Cracow, Poland.ORCID https://orcid.org/0000-0002-9731-908X
Milena GawlińskaDepartment of Physicochemical Drug Analysis, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna St. 9, 30-688, Cracow, Poland.
Paula ZarębaDepartment of Physicochemical Drug Analysis, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna St. 9, 30-688, Cracow, Poland.ORCID https://orcid.org/0000-0002-5037-6183
Agata SiwekDepartment of Pharmacobiology, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna St. 9, 30-688, Cracow, Poland.ORCID https://orcid.org/0000-0001-5321-9266
Małgorzata WolakDepartment of Pharmacobiology, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna St. 9, 30-688, Cracow, Poland.ORCID https://orcid.org/0000-0002-3161-0878
Barbara MordylDepartment of Pharmacobiology, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna St. 9, 30-688, Cracow, Poland.ORCID https://orcid.org/0000-0001-7906-0353
Monika Głuch-LutwinDepartment of Pharmacobiology, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna St. 9, 30-688, Cracow, Poland.ORCID https://orcid.org/0000-0003-1632-6569
Gniewomir LataczDepartment of Technology and Biotechnology of Drugs, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna St. 9, 30-688, Cracow, Poland.ORCID https://orcid.org/0000-0001-9247-2598
Xavier BrazzolottoDépartement de Toxicologie et Risques Chimiques, Institut de Recherche Biomédicale des Armées, 91223, Brétigny sur Orge, France.ORCID https://orcid.org/0000-0001-9219-1032
Fabien ChantegreilDépartement de Toxicologie et Risques Chimiques, Institut de Recherche Biomédicale des Armées, 91223, Brétigny sur Orge, France.ORCID https://orcid.org/0000-0001-5982-8265
Florian NachonDépartement de Toxicologie et Risques Chimiques, Institut de Recherche Biomédicale des Armées, 91223, Brétigny sur Orge, France.ORCID https://orcid.org/0000-0003-0293-2429
Jana Zdarova KarasovaDepartment of Toxicology and Military Pharmacy, Military Faculty of Medicine, University of Defence in Brno, Trebesska 1575, 500 02, Hradec Kralove, Czech Republic.ORCID https://orcid.org/0000-0003-0891-9591
Jaroslav PejchalDepartment of Toxicology and Military Pharmacy, Military Faculty of Medicine, University of Defence in Brno, Trebesska 1575, 500 02, Hradec Kralove, Czech Republic.ORCID https://orcid.org/0000-0003-2228-7922
Martin MzikDepartment of Clinical Biochemistry, University Hospital Hradec Kralove, Sokolska 581, 500 05, Hradec Kralove, Czech Republic.ORCID https://orcid.org/0000-0003-4649-7828
Vit SestakDepartment of Clinical Biochemistry, University Hospital Hradec Kralove, Sokolska 581, 500 05, Hradec Kralove, Czech Republic.ORCID https://orcid.org/0000-0002-4688-2577
Lukas PrchalBiomedical Research Center, University Hospital Hradec Kralove, Sokolska 581, 500 05, Hradec Kralove, Czech Republic.ORCID https://orcid.org/0000-0001-9698-4478
Jitka OdvarkovaDepartment of Toxicology and Military Pharmacy, Military Faculty of Medicine, University of Defence in Brno, Trebesska 1575, 500 02, Hradec Kralove, Czech Republic.ORCID https://orcid.org/0009-0009-0628-9865
Ondrej SoukupDepartment of Toxicology and Military Pharmacy, Military Faculty of Medicine, University of Defence in Brno, Trebesska 1575, 500 02, Hradec Kralove, Czech Republic.ORCID https://orcid.org/0000-0001-6376-8701
Jan KorabecnyDepartment of Toxicology and Military Pharmacy, Military Faculty of Medicine, University of Defence in Brno, Trebesska 1575, 500 02, Hradec Kralove, Czech Republic.ORCID https://orcid.org/0000-0001-6977-7596
Ales SorfDepartment of Toxicology and Military Pharmacy, Military Faculty of Medicine, University of Defence in Brno, Trebesska 1575, 500 02, Hradec Kralove, Czech Republic.ORCID https://orcid.org/0000-0001-7829-3980
Marie HamsikovaDepartment of Chemistry, Faculty of Science, University of Hradec Kralove, Rokitanskeho 62, 500 03, Hradec Kralove, Czech Republic.
Lucie ZemanovaDepartment of Chemistry, Faculty of Science, University of Hradec Kralove, Rokitanskeho 62, 500 03, Hradec Kralove, Czech Republic.ORCID https://orcid.org/0000-0002-2732-5935
Lubica MuckovaBiomedical Research Center, University Hospital Hradec Kralove, Sokolska 581, 500 05, Hradec Kralove, Czech Republic.ORCID https://orcid.org/0000-0001-6693-6061
Nela VánovaDepartment of Pharmaceutical Chemistry and Pharmaceutical Analysis, Faculty of Pharmacy in Hradec Kralove, Charles University, Akademika Heyrovskeho 1203, Hradec Kralove, 500 05, Czech Republic.ORCID https://orcid.org/0000-0002-1827-9308
Pola DryjaDepartment of Pharmacodynamics, Chair of Pharmacodynamics, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna St. 9, 30-688, Cracow, Poland.
Kinga SałatDepartment of Pharmacodynamics, Chair of Pharmacodynamics, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna St. 9, 30-688, Cracow, Poland.ORCID https://orcid.org/0000-0003-0614-5393
Georg HöfnerDepartment of Pharmacy - Center for Drug Research, Ludwig-Maximilians-Universität München, Butenandtstr. 5-13, 81377, Munich, Germany.ORCID https://orcid.org/0000-0002-7957-4503
Klaus WannerDepartment of Pharmacy - Center for Drug Research, Ludwig-Maximilians-Universität München, Butenandtstr. 5-13, 81377, Munich, Germany.ORCID https://orcid.org/0000-0003-4399-1425
Anna WięckowskaDepartment of Physicochemical Drug Analysis, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna St. 9, 30-688, Cracow, Poland.
Barbara MalawskaDepartment of Physicochemical Drug Analysis, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna St. 9, 30-688, Cracow, Poland.ORCID https://orcid.org/0000-0003-4637-5820
Funding
Grantová Agentura České Republiky project No. 22-24384SMinistère des Armées DGA/SSA - NBC-5-C-2316Ministerstvo Obrany České Republiky Project No: DZRO-FVZ22-ZHN IIMinisterstvo Zdravotnictví Ceské Republiky UHHK 00179906Narodowe Centrum Nauki UMO-2021/41/B/NZ7/02825Univerzita Hradec Králové Excellence project no. 2201-2024Univerzita Karlova v Praze SVV 260 666
Abstract
Alzheimer's disease (AD) is a neurodegenerative disorder characterized by memory loss and behavioral and psychological symptoms of dementia (BPSD). Given that cholinergic neurons are predominantly affected in AD, current treatments primarily aim to enhance cholinergic neurotransmission. However, imbalances in other neurotransmitters, such as γ-aminobutyric acid (GABA), also contribute to AD symptomatology. In the presented research, using a combination of crystallography and computational methods we developed compound 6 as a dual modulator of GABAergic and cholinergic neurotransmission systems. Compound 6 demonstrated inhibition of BuChE (IC
Indexed as
Alzheimer DiseaseCholinesterase InhibitorsFluorenesgamma-Aminobutyric AcidSynaptic TransmissionAcetylcholinesteraseAnimalsButyrylcholinesteraseGABA Plasma Membrane Transport ProteinsHumansMiceMolecular StructureAcetylcholinesteraseButyrylcholinesteraseCholinesterase InhibitorsFluorenesGABA Plasma Membrane Transport Proteinsgamma-Aminobutyric AcidAlzheimer's diseasebutyrylcholinesteraseGABA transportersinhibitorsmultitarget drugs
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.