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The search for new substances with anticonvulsant and antinociceptive activity among hybrid compounds based on the pyrrolidine-2,5-dione scaffold

2015/18/E/NZ7/00509

Keywords

Descriptors

  • NZ7_14: Farmacja, farmakoterapia, farmakologia

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)

dr hab. Krzysztof Tomasz Kamiński

Number of co-investigators in the project: 7

Call

SONATA BIS 5 – announced on 2015-06-15

Amount awarded
998 000 PLN
Project start date
2016-04-18
Project end date
2021-04-17
Project duration
60 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. Laptop.
  2. Laptop. Cost: 4 000 PLN
  3. System do chromatografii błyskawicznej (flash) z detektorem ELS/UV/UV-Vis. Cost: 250 000 PLN
  4. System próżniowy z kontrolerem.

Information in the final report

Publication in academic press/journals (7)

  1. Chirality as an important factor for the development of new antiepileptic drugs

    Authors:
    Michał Abram, Marcin Jakubiec, Krzysztof Kamiński
    Academic press:
    ChemMedChem (year: 2019, volume: 14, pages: 1744-1761), Publisher: Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim
    Status:
    Published
    DOI:
    10.1002/cmdc.201900367 – link to the publication

  2. KA-11, a novel pyrrolidine-2,5-dione derived broad-spectrum anticonvulsant: Its antiepileptogenic, antinociceptive properties and in vitro characterization.

    Authors:
    Katarzyna Socała, Szczepan Mogilski, Mateusz Pieróg, Dorota Nieoczym, Michał Abram, Bartłomiej Szulczyk, Annamaria Lubelska, Gniewomir Latacz, Urszula Doboszewska, Piotr Wlaź, Krzysztof Kamiński
    Academic press:
    ACS Chem. Neurosci. (year: 2019, volume: 10, pages: 636−648), Publisher: ACS
    Status:
    Published
    DOI:
    10.1021/acschemneuro.8b00476 – link to the publication

  3. Identification of new compounds with anticonvulsant and antinociceptive properties in a group of 3-substituted (2,5-dioxo-pyrrolidin-1-yl)(phenyl)-acetamides

    Authors:
    Michał Abram, Marcin Jakubiec, Anna Rapacz, Szczepan Mogilski, Gniewomir Latacz, Bartłomiej Szulczyk, Małgorzata Szafarz, Katarzyna Socała, Dorota Nieoczym, Elżbieta Wyska, Piotr Wlaź, Rafał M. Kamiński, and Krzysztof Kamiński
    Academic press:
    International Journal of Molecular Sciences (year: 2021, volume: 22, pages: 13092), Publisher: MDPI
    Status:
    Published
    DOI:
    10.3390/ijms222313092 – link to the publication

  4. Asymmetric synthesis and in vivo/in vitro characterization of new hybrid anticonvulsants derived from (2,5-dioxopyrrolidin-1-yl)phenylacetamides

    Authors:
    Michał Abram, Anna Rapacz, Gniewomir Latacz, Bartłomiej Szulczyk, Justyna Kalinowska-Tłuścik, Dagmara Otto-Ślusarczyk, Marta Struga, Rafał M. Kaminski, Krzysztof Kaminski
    Academic press:
    Bioorganic Chemistry (year: 2021, volume: 109, pages: 104751), Publisher: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.bioorg.2021.104751 – link to the publication

  5. The Search for New Anticonvulsants in a Group of (2,5-Dioxopyrrolidin-1-yl)(Phenyl)Acetamides with Hybrid Structure-Synthesis and In Vivo/In Vitro Studies

    Authors:
    Abram, M.; Jakubiec, M.; Rapacz, A.; Mogilski, S.; Latacz, G.; Kamiński, R. M.; Kamiński, K.
    Academic press:
    International Journal of Molecular Sciences (year: 2020, volume: 21, pages: 8780), Publisher: MDPI
    Status:
    Published
    DOI:
    10.3390/ijms21228780 – link to the publication

  6. Multitargeted Compounds Derived from (2,5-Dioxopyrrolidin-1-yl)(Phenyl)-Acetamides as Candidates for Effective Anticonvulsant and Antinociceptive Agents

    Authors:
    Abram, M.; Rapacz, A.; Mogilski, S.; Latacz, G.; Lubelska, A.; Kamiński, R. M.; Kamiński, K.
    Academic press:
    ACS Chemical Neuroscience (year: 2020, volume: 11, pages: 1996–2008), Publisher: American Chemical Society
    Status:
    Published
    DOI:
    10.1021/acschemneuro.0c00257 – link to the publication

  7. KA-104, a New Multitargeted Anticonvulsant with Potent Antinociceptive Activity in Preclinical Models

    Authors:
    Kamiński, K.; Mogilski, S.; Abram, M.; Rapacz, A.; Latacz, G.; Szulczyk, B.; Walczak, M.; Kuś, K.; Matyjaszczyk, K.; Kamiński, R. M.
    Academic press:
    Epilepsia (year: 2020, volume: 61, pages: 2119–2128), Publisher: Wiley
    Status:
    Published
    DOI:
    10.1111/epi.16669 – link to the publication

Articles in post-conference publications (9)

  1. Hybrid compounds in the search for the new highly effective anticonvulsants

    Authors:
    Michał Abram, Anna Rapacz, Szczepan Mogilski, Gniewomir Latacz, Bartłomiej Szulczyk, Kamil Kuś, Maria Walczak, Krzysztof Kamiński
    Conference:
    14th EILAT Conference on New Antiepileptic Drugs and Devices (ELIAT XIV) (year: 2018, pages: 93-94), Publisher: The Hebrew University of Jerusalem (Israel)
    Date:
    conference 2018.05.13-16
    Status:
    Published

  2. Hybrid compounds based on the pyrrolidine-2,5-dione scaffold as candidates for new wide spectrum anticonvulsant agents

    Authors:
    Krzysztof Kamiński, Michał Abram, Anna Rapacz, Martyna Sojka, Gniewomir Latacz, Jolanta Obniska, Marcin Jakubiec
    Conference:
    14th EILAT Conference on New Antiepileptic Drugs and Devices (ELIAT XIV) (year: 2018, pages: 106-107), Publisher: The Hebrew University of Jerusalem (Israel)
    Date:
    conference 2018.05.13-16
    Status:
    Published

  3. Nowe hybrydowe pochodne pirolidyno-2,5-dionu o silnych właściwościach przeciwdrgawkowych i przeciwbólowych w badaniach przedklinicznych

    Authors:
    Krzysztof Kamiński, Michał Abram, Marcin Jakubiec, Anna Rapacz, Szczepan Mogilski, Gniewomir Latacz, Bartłomiej Szulczyk
    Conference:
    IV Sympozjum Szkoła Chemii Medycznej (year: 2019, pages: 53), Publisher: Uniwersytet Medyczny im. Piastów Śląskich we Wrocławiu
    Date:
    conference 25-27.09.2019
    Status:
    Published

  4. New hybrid derivatives of 2-(2,5-dioxopyrrolidin-1-yl)-2-phenylacetamide with anticonvulsant and antinociceptive properties in the preclinical studies

    Authors:
    Michał Abram, Marcin Jakubiec, Anna Rapacz, Szczepan Mogilski, Gniewomir Latacz, Krzysztof Kamiński
    Conference:
    EFMC-ACSMEDI MedChem Frontiers 2019 (year: 2019, pages: 99), Publisher: European Federation for Medicinal Chemistry
    Date:
    conference 10-13.06.2019
    Status:
    Published

  5. KA-104, a novel hybrid molecule as promising candidate for new highly effective anticonvulsant

    Authors:
    Michał Abram, Marcin Jakubic, Anna Rapacz, Szczepan Mogilski,Gniewomir Latacz, Bartłomiej Szulczyk, Krzysztof Kamiński
    Conference:
    XI Multidyscyplinarna Konferencja Nauki o Leku Nauka Dla Przemysłu (year: 2018, pages: 151 (P64)), Publisher: Instytut Farmaceutyczny w Warszawie
    Date:
    conference 2018.11.14-16
    Status:
    Published

  6. Hybrid compounds in the search for the new highly effective anticonvulsants

    Authors:
    Krzysztof Kamiński
    Conference:
    The 10th Joint Meeting on Medicinal Chemistry 2017 (year: 2017, pages: 52), Publisher: Croatian Chemical Society
    Date:
    conference 2017.06.25-28
    Status:
    Published

  7. Związki hybrydowe pochodne kwasu (2,5-dioksopirolidyn-1-ylo)(fenylo)octowego o szerokim działaniu ochronnym w zwierzęcych modelach padaczki

    Authors:
    Michał Abram, Anna Rapacz, Krzysztof Kamiński
    Conference:
    VII Konferencja Doktorantów Uniwersytetu Jagiellońskiego – Collegium Medicum (year: 2017, pages: 46211), Publisher: Uniwersytetu Jagiellońskiego – Collegium Medicum
    Date:
    conference 2017.05.27
    Status:
    Published

  8. Związki hybrydowe pochodne pirolidyno-2,5-dionu w poszukiwaniu wysoce efektywnych leków przeciwpadaczkowych

    Authors:
    Michał Abram, Anna Rapacz, Jolanta Obniska, Barbara Filipek, Krzysztof Kamiński
    Conference:
    XXIII NAUKOWY ZJAZD POLSKIEGO TOWARZYSTWA FARMACEUTYCZNEGO (year: 2017, pages: 290), Publisher: Copyright by Polskie Towarzystwo Farmaceutyczne (ISBN 978-83-942760-4-1)
    Date:
    conference 2017.09.19-22
    Status:
    Published

  9. The search for new broad-spectrum anticonvulsants in a group of hybrid compounds derived from N-benzyl-2-(2,5-dioxopyrrolidin-1-yl)-2-phenylacetamide

    Authors:
    Michał Abram, Anna Rapacz, Krzysztof Kamiński
    Conference:
    IX Konwersatorium Chemii Medycznej (year: 2018, pages: 57 (P1)), Publisher: Uniwersytet Medyczny w Lublinie
    Date:
    conference 2018.09.13-15
    Status:
    Published

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Graphic design and implementation: Jakub Piotrowski