Projects funded by the NCN

Information on the principal investigator and host institution

Information of the project and the call

Keywords

Equipment

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Novel multi-target directed ligands combining cholinesterase inhibition and 5-HT6 antagonism - design, synthesis and pharmacological evaluation of compounds with potential procognitive activity.

2016/23/D/NZ7/01328

Keywords:

multi-target-directed ligands 5-HT6 receptor antagonists cholinesterase inhibitors drug design

Descriptors:

  • ST5_23:
  • NZ7_14: Pharmacy, pharmacotherapy, pharmacology

Panel:

NZ7 - Diagnostic tools, therapies and public health: public health, epidemiology, environmental health risks and occupational medicine, medical ethics, drug discovery and therapies, pharmacology

Host institution :

Uniwersytet Jagielloński - Collegium Medicum, Collegium Medicum, Wydział Farmaceutyczny

woj. małopolskie

Other projects carried out by the institution 

Principal investigator (from the host institution):

dr hab. Anna Więckowska 

Number of co-investigators in the project: 7

Call: SONATA 12 - announced on 2016-09-15

Amount awarded: 582 250 PLN

Project start date (Y-m-d): 2017-08-04

Project end date (Y-m-d): 2022-02-03

Project duration:: 54 months (the same as in the proposal)

Project status: Project settled

Project description

Download the project description in a pdf file

Note - project descriptions were prepared by the authors of the applications themselves and placed in the system in an unchanged form.

Equipment purchased [PL]

  1. Wirówka z rotorem (7 092 PLN)
  2. Small-Molecule Drug Discovery Suite (Schrödinger LLC) - licencja na oprogramowanie (20 000 PLN)
  3. Worteks (4 247 PLN)

Information in the final report

  • Publication in academic press/journals (6)
  • Articles in post-conference publications (5)
  1. Development and crystallography-aided SAR studies of multifunctional BuChE inhibitors and 5-HT6R antagonists with β-amyloid anti-aggregation properties
    Authors:
    Tomasz Wichur, Justyna Godyń, Izabella Góral, Gniewomir Latacz, Adam Bucki, Agata Siwek, Monika Głuch-Lutwin, Barbara Mordyl, Joanna Śniecikowska, Maria Walczak, Damijan Knez, Marko Jukic, Kinga Sałat, Stanislav Gobec, Marcin Kołaczkowski, Barbara Malawska, Xavier Brazzolotto, Anna Więckowska
    Academic press:
    European Journal of Medicinal Chemistry (rok: 2021, tom: 225, strony: 113792), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2021.113792 - link to the publication
  2. In Vitro and In Silico ADME-Tox Profiling and Safety Significance of Multifunctional Monoamine Oxidase Inhibitors Targeting Neurodegenerative Diseases
    Authors:
    Więckowska, A.; Szałaj, N.; Góral, I.; Bucki, A.; Latacz, G.; Kiec-Kononowicz, K.; Bautista-Aguilera O-M.; Romero, A.; Ramos, E.; Egea, J.; Farré Alíns, V.; González-Rodríguez, A.; López-Munoz, F.; Chioua, M.; Marco-Contelles, J.
    Academic press:
    ACS Chemical Neuroscience (rok: 2020, tom: 11, strony: 3793-3801), Wydawca: ACS Publications
    Status:
    Published
    DOI:
    10.1021/acschemneuro.0c00489 - link to the publication
  3. Multidirectional in vitro and in cellulo studies as a tool for identification of multi-target-directed ligands aiming at symptoms and causes of Alzheimer's disease
    Authors:
    Szałaj, N.; Godyń, J.; Jończyk, J.; Pasieka, A.; Panek, D.; Wichur, T.; Więckowski, K.; Zaręba, P.; Bajda, M.; Pislar, A.; Malawska, B.; Sabate, R.; Więckowska, A.
    Academic press:
    Journal of Enzyme Inhibition and Medicinal Chemistry (rok: 2020, tom: 35, strony: 1944-1952), Wydawca: Taylor & Francis Online
    Status:
    Published
    DOI:
    10.1080/14756366.2020.1835882 - link to the publication
  4. Novel Multitarget-Directed Ligands Aiming at Symptoms and Causes of Alzheimer's Disease
    Authors:
    Anna Więckowska, Tomasz Wichur, Justyna Godyń, Adam Bucki, Monika Marcinkowska, Agata Siwek, Krzysztof Więckowski, Paula Zaręba, Damijan Knez, Monika Głuch-Lutwin, Grzegorz Kazek, Gniewomir Latacz, Kamil Mika, Marcin Kołaczkowski, Jan Korabecny, Ondrej Soukup, Marketa Benkova, Katarzyna Kieć-Kononowicz, Stanislav Gobec, Barbara Malawska
    Academic press:
    ACS Chemical Neuroscience (rok: 2018, tom: 9, strony: 1195-1214), Wydawca: ACS Publications
    Status:
    Published
    DOI:
    10.1021/acschemneuro.8b00024 - link to the publication
  5. Anti-Alzheimer's Multi-Target-Directed Ligands with Serotonin 5-HT6 Antagonist, Butyrylcholinesterase Inhibitory and Antioxidant Activity
    Authors:
    Monika Marcinkowska, Adam Bucki, Dawid Panek, Agata Siwek, Nikola Fajkis, Marek Bednarski, Małgorzata Zygmunt, Magdalena Kotańska, Marcin Kołaczkowski, Anna Więckowska
    Academic press:
    Archiv der Pharmazie (rok: 2019, tom: 352, strony: 1900041), Wydawca: Wiley Online Library
    Status:
    Published
    DOI:
    10.1002/ardp.201900041 - link to the publication
  6. Discovery of 1-(phenylsulfonyl)-1H-indole-based multifunctional ligands targeting cholinesterases and 5-HT6 receptor with anti-aggregation properties against amyloid-beta and tau
    Authors:
    Tomasz Wichur, Anna Pasieka, Justyna Godyń, Dawid Panek, Izabella Góral, Gniewomir Latacz, Ewelina Honkisz-Orzechowska, Adam Bucki, Agata Siwek, Monika Głuch-Lutwin, Damijan Knez, Xavier Brazzolotto, Stanislav Gobec, Marcin Kołaczkowski, Raimon Sabate, Anna Więckowska
    Academic press:
    European Journal of Medicinal Chemistry (rok: 2021, tom: 225, strony: 113783), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2021.113783 - link to the publication
  1. Multifunctional ligands targeting cholinesterases, 5-HT6 receptors and β-amyloid
    Authors:
    Anna Więckowska, Barbara Malawska
    Conference:
    3rd Annual meeting | MuTaLig Cost Action (rok: 2018, ), Wydawca: www.mutalig.eu
    Data:
    konferencja 18-19.10.2018
    Status:
    Published
    DOI:
    link to the publication
  2. Targeting serotoninergic system, cholinesterases and amyloid-beta aggregation in the search for effective treatment of Alzheimer's disease
    Authors:
    Tomasz Wichur, Justyna Godyń, Agata Siwek, Monika Głuch-Lutwin, Damijan Knez, Adam Bucki, Marcin Kołaczkowski, Stanislav Gobec, Barbara Malawska, Anna Więckowska
    Conference:
    Medicinal Chemistry Frontiers 2019 (rok: 2019, ), Wydawca: www.medchemfrontiers.org
    Data:
    konferencja 43626
    Status:
    Published
  3. MULTI-TARGET-DIRECTED LIGANDS WITH POTENTIAL DISEASE MODIFYING AND SYMPTOMATIC EFFECTS IN ALZHEIMER'S DISEASE
    Authors:
    Anna Wieckowska, Tomasz Wichur, Justyna Godyn, Dawid Panek, Jakub Jonczyk, Krzysztof Wieckowski, Damijan Knez, Stanislav Gobec, Marcin Kolaczkowski, Adam Bucki, Monika Marcinkowska, Barbara Malawska
    Conference:
    EFMC-ISMC 2018 XXV EFMC International Symposium on Medicinal Chemistry (rok: 2018, ), Wydawca: -
    Data:
    konferencja 2-6.09.2018
    Status:
    Published
  4. Multifunctional ligands combining 5-HT6 receptor antagonism, inhibition of chelinesterases and beta-amyloid aggregation as potential disease-modifying agents against Alzheimer's disease
    Authors:
    Wichur T, Godyń J., Głuch-Lutwin M., Knez D., Bucki A., Kołaczkowski M., Gobec S., Malawska B., Więckowska A.
    Conference:
    Mendeleev 2019, XI International Conference on Chemistry for Young Scientists (rok: 2019, ), Wydawca: http://mendeleev2019.ru/index.php/en/
    Data:
    konferencja 43717
    Status:
    Published
  5. Serotonin 5-HT6 receptor antagonists and cholinesterase inhibitors with amyloid beta antiaggregation properties in the development of multifunctional ligands against Alzheimer's disease
    Authors:
    Anna Więckowska
    Conference:
    Joint Meeting on Medicinal Chemistry (rok: 2019, ), Wydawca: Guarant International spol. s.r.o.
    Data:
    konferencja 43643
    Status:
    Published

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