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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

Descriptors

  • NZ7_14: Farmacja, farmakoterapia, farmakologia
  • ST5_16: Chemia biologiczna
  • NZ7_16: Inne zagadnienia pokrewne

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

Voivodeship: małopolskie

Other projects carried out by the institution »

Principal investigator (from the host institution)

prof. Barbara Antonina 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
2017-01-24
Project end date
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. Aparat do preparatywnej chromatografii cieczowej. Cost: 360 000 PLN
  2. Komputer stacjonarny.
  3. Monitor do komputera.
  4. Oprogramowanie komputerowe. Cost: 12 000 PLN
  5. Pipeta elektroniczna.
  6. Prekolumny do aparatu HPLC.
  7. Przedkolumna + uchwyt (do aparatu HPLC).
  8. Waga precyzyjna ENTRIS. Cost: 7 218 PLN

Information in the final report

Publication in academic press/journals (8)

  1. 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 (year: 2020, volume: 217, pages: 121023), Publisher: 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

  2. 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 (year: 2018, volume: 11, pages: 33), Publisher: American Chemical Society
    Status:
    Published

  3. 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 (year: 2020, volume: 187, pages: 11916), Publisher: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2019.111916 – link to the publication

  4. 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 (year: 2017, volume: Vol 9, nr 15, pages: 1835-1854), Publisher: Newlands Press Future Science Group
    Status:
    Published

  5. 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) (year: 2021, volume: WO2021/235956A2, pages: 25569), Publisher: World Intelectual Property Organization
    Status:
    Published

  6. 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 (year: 2018, volume: 23, pages: 347), Publisher: MDPI AG
    Status:
    Published
    DOI:
    10.3390/molecules23020347 – link to the publication

  7. 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 (year: 2021, volume: 12, pages: 2057−2068), Publisher: American Chemical Society
    Status:
    Published
    DOI:
    10.1021/acschemneuro.1c00235 – link to the publication

  8. 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 (year: 2021, volume: 218, pages: 113397), Publisher: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2021.113397 – link to the publication

Articles in post-conference publications (1)

  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. (year: 2017, pages: Suppl vol 13, 7, P280), Publisher: Elsevier for the Alzheimer's Association
    Date:
    conference 16-20-07-2017
    Status:
    Published

Book publications / chapters in book publications (1)

  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 (year: 2020, volume: 1, pages: 181-203), Publisher: Exon Publications; ISBN: 978-0-6450017-0-9
    Status:
    Published

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