Projects funded by the NCN


Information on the principal investigator and host institution

Information of the project and the call

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Multifunctional ligands - TRPA1 channel antagonists and phosphodiesterases inhibitors as a new approach for the treatment of pain and chronic respiratory disorders

2018/29/B/NZ7/00285

Keywords:

neuropathic pain chronic respiratory disorders

Descriptors:

  • ST5_16:
  • 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. Grażyna Chłoń-Rzepa 

Number of co-investigators in the project: 16

Call: OPUS 15 - announced on 2018-03-15

Amount awarded: 1 264 800 PLN

Project start date (Y-m-d): 2019-01-21

Project end date (Y-m-d): 2024-01-20

Project duration:: 36 months (the same as in the proposal)

Project status: Project completed

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.

Information in the final report

  • Publication in academic press/journals (7)
  • Articles in post-conference publications (6)
  1. Evaluation of analgesic and anti-inflammatory activity of purine-2,6-dione-based TRPA1 antagonists with PDE4/7 inhibitory activity
    Authors:
    Małgorzata Zygmunt, Marietta Ślusarczyk, Agnieszka Jankowska, Artur Świerczek, Adrian Bryła, Szczepan Mogilski, Grzegorz Kazek, Jacek Sapa, Elżbieta Wyska, Grażyna Chłoń-Rzepa
    Academic press:
    Pharmacological Reports (rok: 2022, tom: 74, strony: 982-997), Wydawca: Springer
    Status:
    Published
    DOI:
    10.1007/s43440-022-00397-6 - link to the publication
  2. Estimation of the lipophilicity of purine-2,6-dione-based TRPA1 antagonists and PDE4/7 inhibitors with analgesic activity
    Authors:
    Monika Dąbrowska, Małgorzata Starek, Grażyna Chłoń-Rzepa, Agnieszka Zagórska, Łukasz Komsta, Agnieszka Jankowska, Marietta Ślusarczyk, Maciej Pawłowski
    Academic press:
    Bioorganic & Medicinal Chemistry Letters (rok: 2021, tom: 49, strony: 128318), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.bmcl.2021.128318 - link to the publication
  3. Analgesic and Anti-inflammatory activity of new analogs of HC-030031: a TRPA1 channel antagonist
    Authors:
    Adrian Bryła, Marietta Ślusarczyk, Małgorzata Zygmunt, Grażyna Chłoń-Rzepa, Grzegorz Kazek
    Academic press:
    Acta Poloniae Pharmaceutica (rok: 2020, tom: 77, strony: 113-119), Wydawca: Polskie Towarzystwo Farmaceutyczne
    Status:
    Published
    DOI:
    10.32383/appdr/117836 - link to the publication
  4. Multifunctional Ligands Targeting Phosphodiesterase as the Future Strategy for the Symptomatic and Disease-Modifying Treatment of Alzheimer's Disease
    Authors:
    Agnieszka Jankowska, Anna Wesołowska, Maciej Pawłowski and Grażyna Chłoń-Rzepa
    Academic press:
    Current Medicinal Chemistry (rok: 2020, tom: 27, strony: 5351-5373), Wydawca: Bentham Science
    Status:
    Published
    DOI:
    10.2174/0929867326666190620095623 - link to the publication
  5. Diabetic Theory in Anti-Alzheimer's Drug Research and Development. Part 2: Therapeutic Potential of Camp-Specific Phosphodiesterase Inhibitors
    Authors:
    Agnieszka Jankowska, Maciej Pawłowski, Grażyna Chłoń-Rzepa
    Academic press:
    Current Medicinal Chemistry (rok: 2021, tom: 28, strony: 3535-3553), Wydawca: Bentham Science
    Status:
    Published
    DOI:
    10.2174/0929867327666200917125857 - link to the publication
  6. A Novel, Pan-PDE Inhibitor Exerts Anti-Fibrotic Effects in Human Lung Fibroblasts via Inhibition of TGF-β Signaling and Activation of cAMP/PKA Signaling
    Authors:
    Katarzyna Wójcik-Pszczoła, Grażyna Chłoń-Rzepa , Agnieszka Jankowska, Marietta Ślusarczyk, Paweł E. Ferdek, Agnieszka A. Kusiak, Artur Świerczek, Krzysztof Pociecha, Paulina Koczurkiewicz-Adamczyk, Elżbieta Wyska, Elżbieta Pękala, Reinoud Gosens
    Academic press:
    International Journal of Molecular Sciences (rok: 2020, tom: 21, strony: 4008), Wydawca: Multidisciplinary Digital Publishing Institute (MDPI)
    Status:
    Published
    DOI:
    10.3390/ijms21114008 - link to the publication
  7. Advances in the Discoveryof PDE10A Inhibitors for CNS-Related Disorders. Part 2: Focus on Schizophrenia
    Authors:
    Artur Świerczek, Agnieszka Jankowska, Grażyna Chłoń-Rzepa, Maciej Pawłowski, Elżbieta Wyska
    Academic press:
    Current Drug Targets (rok: 2019, tom: 20, strony: 1652-1669), Wydawca: Bentham Science
    Status:
    Published
    DOI:
    10.2174/1389450120666190801114210 - link to the publication
  1. A new class of purine-2,6-dione-based TRPA1 antagonists: molecular modeling study and analgesic activity in animal pain models.
    Authors:
    Grażyna Chłoń-Rzepa, Alicja Gawalska, Krzysztof Więckowski, Beata Gryzło, Adam Bucki, Grzegorz Kazek, Katarzyna Urbańska, Kinga Sałat
    Conference:
    57th International Conference on Medicinal Chemistry (rok: 2023, ), Wydawca: Societe de Chimie Therapeutique
    Data:
    konferencja 05-07.07.2023
    Status:
    Published
  2. Novel purine-2,6-dione-based multifunctional PDE inhibitors and TRPA1 antagonists as a new approach for treating chronic airway diseases
    Authors:
    Grażyna Chłoń-Rzepa, Katarzyna Wójcik-Pszczoła, Marietta Ślusarczyk, Agnieszka Jankowska, Alicja Gawalska, Adam Bucki, Artur Świerczek, Krzysztof Pociecha, Elżbieta Wyska, Krzysztof Więckowski, Beata Gryzło, Grzegorz Kazek, Maciej Pawłowski
    Conference:
    X Konwersatorium Chemii Medycznej (rok: 2021, ), Wydawca: Polskie Towarzystwo Chemii Medycznej
    Data:
    konferencja 03-05.09.2021
    Status:
    Published
  3. New Class of TRPA1 antagonists and/or PDE inhibitors based on purine-2,6-dione scaffold as potential analgesic agents
    Authors:
    Grażyna Chłoń-Rzepa, Marietta Ślusarczyk, Agnieszka Jankowska, Adam Bucki, Alicja Gawalska, Maciej Pawlowski, Artur Świerczek, Krzysztof Pociecha, Elżbieta Wyska, Małgorzata Zygmunt, Grzegorz Kazek
    Conference:
    Joint Meeting on Medicinal Chemistry (rok: 2019, ), Wydawca: GUARANT International spol. s r.o.
    Data:
    konferencja 27-30.06.2019
    Status:
    Published
  4. Trisubstituted triazines as multifunctional TRPA1/PDEs ligands: Synthesis, pharmacological evaluation and molecular modeling study.
    Authors:
    Paweł Żmudzki, Alicja Gawalska, Artur Świerczek, Krzysztof Pociecha, Katarzyna Wójcik-Pszczoła, Kamil Piska, Natalia Kocot, Grzegorz Kazek, Elżbieta Wyska, Grażyna Chłoń-Rzepa
    Conference:
    XI Konwersatorium Chemii Medycznej (rok: 2023, ), Wydawca: Polskie Towarzystwo Chemii Medycznej
    Data:
    konferencja 14-16.09.2023
    Status:
    Published
  5. 8-Alkylamine derivatives of purine-2,6-dione as PDE inhibitors and TRPA1 antagonists: a novel approach for the treatment of chronic respiratory diseases
    Authors:
    G. Chłoń-Rzepa, A. Jankowska, M. Ślusarczyk, K. Wójcik-Pszczoła, A. Świerczek, K. Pociecha, E. Wyska, G. Kazek, M. Pawłowski
    Conference:
    3rd International Conference on Pharmaceutical and Medical Science (rok: 2020, ), Wydawca: ZOZ Ośrodek UMEA SHINODA-KURACEJO
    Data:
    konferencja 24-26.09.2020
    Status:
    Published
  6. Anti-fibrotic effect of novel purine-2,6-dione-based multifunctional PDEs inhibitors and TRPA1 antagonists as a perspective treatment for chronic airway disorders
    Authors:
    Grażyna Chłoń-Rzepa, Katarzyna Wójcik-Pszczoła, Marietta Ślusarczyk, Agnieszka Jankowska, Alicja Gawalska, Adam Bucki, Artur Świerczek, Krzysztof Pociecha, Elżbieta Wyska, Krzysztof Więckowski, Beata Gryzło, Grzegorz Kazek
    Conference:
    EFMC-ISMC International Symposium on Medicinal Chemistry (rok: 2022, ), Wydawca: EFMC
    Data:
    konferencja 04-08.09.2022
    Status:
    Published