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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Multifunctional inhibitors of beta-secretase with anti-aggregating properties of neurotoxic peptides - beta-amyloid and tau protein.

2016/21/B/NZ7/01744

Keywords:

multi-target-directed ligands molecular modeling beta-secretase inhibitors beta-amyloid inhibition tau inhibitors Alzheimer's disease

Descriptors:

  • NZ7_14: Pharmacy, pharmacotherapy, pharmacology
  • ST5_16:
  • NZ7_16: Other related subjects

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):

prof. Barbara Malawska 

Number of co-investigators in the project: 9

Call: OPUS 11 - announced on 2016-03-15

Amount awarded: 1 295 000 PLN

Project start date (Y-m-d): 2017-01-24

Project end date (Y-m-d): 2021-04-23

Project duration:: 51 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. Komputer stacjonarny.
  2. Waga precyzyjna ENTRIS (7 218 PLN)
  3. Aparat do preparatywnej chromatografii cieczowej (360 000 PLN)
  4. Oprogramowanie komputerowe (12 000 PLN)
  5. Monitor do komputera.
  6. Prekolumny do aparatu HPLC.
  7. Przedkolumna + uchwyt (do aparatu HPLC).
  8. Pipeta elektroniczna.

Information in the final report

  • Publication in academic press/journals (8)
  • Articles in post-conference publications (1)
  • Book publications / chapters in book publications (1)
  1. Advances toward multifunctional cholinesterase and β-amyloid aggregation inhibitors
    Authors:
    Dawid Panek, Tomasz Wichur, Justyna Godyń, Anna Pasieka, Barbara Malawska
    Academic press:
    Future Medicinal Chemistry (rok: 2017, tom: Vol 9, nr 15, strony: 1835-1854), Wydawca: Newlands Press Future Science Group
    Status:
    Published
    DOI:
    brak - link to the publication
  2. Discovery of multifunctional anti-Alzheimer's agents with a unique mechanism of action including inhibition of the enzyme butyrylcholinesterase and γ-aminobutyric acid transporters
    Authors:
    A. Pasieka, D. Panek, J. Jończyk, J. Godyń, N. Szałaj, G. Latacz, J. Tabor, E. Mezeiova, F. Chantegreil, J. Dias, D. Knez, J. Lu, R. Pi, J. Korabecny, X. Brazzolotto, S. Gobec, G. Höfner, K. Wanner, A. Więckowska, B. Malawska
    Academic press:
    European Journal of Medicinal Chemistry (rok: 2021, tom: 218, strony: 113397), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2021.113397 - link to the publication
  3. Design, Synthesis, and Biological Evaluation of 2-(Benzylamino-2-Hydroxyalkyl)Isoindoline-1,3-Diones Derivatives as Potential Disease-Modifying Multifunctional Anti-Alzheimer Agents
    Authors:
    Dawid Panek , Anna Więckowska, Anna Pasieka, Justyna Godyń, Jakub Jończyk, Marek Bajda, Damijan Knez, Stanislav Gobec, and Barbara Malawska
    Academic press:
    Molecules (rok: 2018, tom: 23, strony: 347), Wydawca: MDPI AG
    Status:
    Published
    DOI:
    10.3390/molecules23020347 - link to the publication
  4. Dual inhibitors of amyloid-β and tau aggregation with amyloid-β disaggregating properties: extended in cellulo, in silico and kinetic studies of multifunctional anti-Alzheimer's agents
    Authors:
    Anna Pasieka, Dawid Panek, Natalia Szałaj, Alba Espargaró, Anna Więckowska, Barbara Malawska, Raimon Sabaté, Marek Bajda
    Academic press:
    ACS Chemical Neuroscience (rok: 2021, tom: 12, strony: 2057−2068), Wydawca: American Chemical Society
    Status:
    Published
    DOI:
    10.1021/acschemneuro.1c00235 - link to the publication
  5. 1-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease
    Authors:
    Tomasz Wichur, Anna Więckowska, Krzysztof Więckowski, Justyna Godyń, Jakub Jończyk, Álvaro del Río Valdivieso, Dawid Panek, Anna Pasieka, Raimon Sabaté, Damijan Knez, Stanislav Gobec, and Barbara Malawska
    Academic press:
    European Journal of Medicinal Chemistry (rok: 2020, tom: 187, strony: 11916), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2019.111916 - link to the publication
  6. Design, synthesis and biological evaluation of 1-benzylamino-2-hydroxyalkyl derivatives as new potential disease-modifying multifunctional anti-Alzheimer's agents
    Authors:
    Dawid Panek, Anna Więckowska, Jakub Jończyk, Justyna Godyń, Marek Bajda, Tomasz Wichur, Anna Pasieka, Damijan Knez, Anja Pišlar, Jan Korabecny, Ondrej Soukup, Vendula Sepsova, Raimon Sabaté, Janko Kos, Stanislav Gobec, Barbara Malawska
    Academic press:
    ACS Chemical Neuroscience (rok: 2018, tom: 11, strony: 33), Wydawca: American Chemical Society
    Status:
    Published
    DOI:
    brak - link to the publication
  7. Novel 9H-fluorene derivatives or their pharmaceutically acceptable salts
    Authors:
    Dawid Panek, Barbara Malawska, Anna Pasieka, Jakub Jończyk, Anna Więckowska, Justyna Godyń, Natalia Szałaj, Marek Bajda, Kinga Sałat
    Academic press:
    INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (rok: 2021, tom: WO2021/235956A2, strony: 25569), Wydawca: World Intelectual Property Organization
    Status:
    Published
    DOI:
    brak - link to the publication
  8. Novel application of capillary electrophoresis with a liposome coatedcapillary for prediction of blood-brain barrier permeability
    Authors:
    Justyna Godyń, Dominika Gucwa, Tereza Kobrlova, Martin Novak, Ondrej Soukup,Barbara Malawska, Marek Bajda
    Academic press:
    Talanta (rok: 2020, tom: 217, strony: 121023), Wydawca: Published by Elsevier B.V. This is an open access article under the CC BY license
    Status:
    Published
    DOI:
    10.1016/j.talanta.2020.121023 - link to the publication
  1. Design, synthesis and biological evaluation of novel benzylamine derivatives with hydroxyethylamine pharmacophoric moiety as multifunctional compounds targeting cholinesterase, beta-secretase and beta-amyloid aggregation
    Authors:
    Barbara Malawska, Dawid Panek, Anna Wieckowska, Justyna Godyn, Jakub Jonczyk, Marek Bajda, Damijan Knez, Stanislav Gobec
    Conference:
    Alzheimer's Association International Conference® 2017 (AAIC®) in London, England. (rok: 2017, ), Wydawca: Elsevier for the Alzheimer's Association
    Data:
    konferencja 16-20-07-2017
    Status:
    Published
  1. Multifunctional Ligand Approach: Search for Effective Therapy Against Alzheimer's Disease
    Authors:
    Anna Pasieka, Dawid Panek, Barbara Malawska
    Book:
    Alzheimer's Disease: Drug Discovery (rok: 2020, tom: 1, strony: 181-203), Wydawca: Exon Publications; ISBN: 978-0-6450017-0-9
    Status:
    Published

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