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New selective antagonists of ionotropic glutamate non-NMDA receptors

2014/15/B/NZ7/00908

Keywords

Descriptors

  • NZ7_14: Farmacja, farmakoterapia, farmakologia
  • NZ4_7: Neurofizjologia
  • NZ3_7: Przekaźnictwo sygnału

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 Ewa Monika Szymańska

Number of co-investigators in the project: 7

Call

OPUS 8 – announced on 2014-09-15

Amount awarded
718 730 PLN
Project start date
2015-07-14
Project end date
2019-06-13
Project duration
47 months (the same as in the proposal)
Project status
Project settled

Equipment purchased [PL]

  1. Chłodziarka laboratoryjna.
  2. Klawiatura. Cost: 599 PLN
  3. Komputer stacjonarny. Cost: 6 248 PLN
  4. Kości pamięci. Cost: 1 095 PLN
  5. Laptop.
  6. Meszadło magnetyczne.
  7. Mieszadło magnetyczne do syntezy z termometrem kontaktowym (2 pcs). Cost: 10 000 PLN
  8. Pompa membranowa do wyparki. Cost: 30 000 PLN
  9. Schrodinger Suite (2-letnia licencja) lub inne profesjonalne oprogramowanie do modelowania i dokowania molekularnego (2 pcs). Cost: 50 000 PLN
  10. Urządzenie do chłodzenia cieczy w chłodnicy wyparki. Cost: 15 000 PLN
  11. Urządzenie do pomiaru siły mięśniowej. Cost: 21 000 PLN
  12. Łażnia wodna z termostatem. Cost: 5 000 PLN

Information in the final report

Publication in academic press/journals (5)

  1. Studies on aryl-substituted phenylalanines: Synthesis, activity, and different binding modes at AMPA receptors

    Authors:
    E. Szymańska, K. Frydenvang, D.S. Pickering, C. Krintel, B. Nielsen, A. Kooshki, L.G. Zachariassen, L. Olsen, J.S. Kastrup, T.N. Johansen
    Academic press:
    Journal of Medicinal Chemistry (year: 2016, volume: 59, pages: 448-461), Publisher: ACS Publications
    Status:
    Published
    DOI:
    10.1021/acs.jmedchem.5b01666 – link to the publication

  2. Design, synthesis and structure-activity relationships of novel phenylalanine-based amino acids as kainate receptors ligands

    Authors:
    E. Szymańska, P. Chałupnik, K. Szczepańska, A.M.C. Moral, D.S. Pickering, B. Nielsen, T.N. Johansen, K. Kieć-Kononowicz
    Academic press:
    Bioorganic and Medicinal Chemistry Letters (year: 2016, volume: 26, pages: 5568-5572), Publisher: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.bmcl.2016.09.075 – link to the publication

  3. Phenylalanine derivatives with modulating effects on human α1-glycine receptors and anticonvulsant activity in strychnine-induced seizure model in male adult rats

    Authors:
    B. Sadek, M. Oz, S.M. Nurulain, P. Jayaprakash, G. Latacz, K. Kieć-Kononowicz, E. Szymańska
    Academic press:
    Epilepsy Research (year: 2017, volume: 138, pages: 124-131), Publisher: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.eplepsyres.2017.05.008 – link to the publication

  4. Pharmacological characterization and binding modes of novel racemic and optically active phenylalanine-based antagonists of AMPA receptors

    Authors:
    E. Szymańska, B. Nielsen, T.N. Johansen, A.M. Cuñado Moral, D.S. Pickering, K. Szczepańska, A. Mickowska, K. Kieć-Kononowicz
    Academic press:
    European Journal of Medicinal Chemistry (year: 2017, volume: 138, pages: 874-883), Publisher: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2017.07.007 – link to the publication

  5. Aryl- and heteroaryl-substituted phenylalanines as AMPA receptor ligands

    Authors:
    E. Szymańska, P. Chałupnik, T.N. Johansen, B. Nielsen, A.M. Cuñado Moral, D.S. Pickering, A. Więckowska, K. Kieć-Kononowicz
    Academic press:
    Chemical Biology & Drug Design (year: 2017, volume: 90, pages: 1271-1281), Publisher: Wiley
    Status:
    Published
    DOI:
    10.1111/cbdd.13048 – link to the publication

Articles in post-conference publications (10)

  1. Design, synthesis and molecular modeling of potential ligands for ionotropic glutamate receptors

    Authors:
    P. Chałupnik, E. Szymańska
    Conference:
    11th Joint Meeting on Medicinal Chemistry 2019 (year: 2019, pages: 56), Publisher: Faculty of Pharmacy in Hradec Kralove, Charles University, Czech Republic
    Date:
    conference 27-30.06
    Status:
    Published

  2. Design, synthesis and molecular modeling of potential ligands of ionotropic glutamate receptors

    Authors:
    P. Chałupnik, E. Szymańska
    Conference:
    XII Copernican International Young Scientist Conference (year: 2018, pages: 96), Publisher: Uniwersytet Mikołaja Kopernika w Toruniu
    Date:
    conference 28-29.06
    Status:
    Published

  3. Phenylalanine-based amino acids as AMPA receptor antagonists

    Authors:
    P. Chałupnik, E. Szymańska, T.N. Johansen, B. Nielsen, A.M. Cuñado Moral, D.S. Pickering, K. Kieć-Kononowicz
    Conference:
    VIII Konwersatorium Chemii Medycznej (year: 2016, pages: P87), Publisher: Polskie Towarzystwo Chemii Medycznej
    Date:
    conference 15-17.09
    Status:
    Published

  4. Synteza i modelowanie komputerowe selektywnych ligandów jonotropowych receptorów kwasu glutaminowego

    Authors:
    P. Chałupnik, E. Szymańska
    Conference:
    III Sympozjum Szkoła Chemii Medycznej (year: 2017, pages: PP66), Publisher: Uniwersytet Medyczny im. Piastów Śląskich we Wrocławiu
    Date:
    conference 6-8.09
    Status:
    Published

  5. Studies on aryl-substituted phenylalanines: Synthesis, activity and different binding modes at AMPA receptors

    Authors:
    E. Szymańska, B. Nielsen, D. Pickering, T.N. Johansen
    Conference:
    10th Joint Meeting on Medicinal Chemistry (year: 2017, pages: 225), Publisher: Croatian Chemical Society, Zagreb, Croatia
    Date:
    conference 25-28.06
    Status:
    Published

  6. Design, synthesis and molecular modeling of potential ligands of ionotropic glutamate receptors

    Authors:
    E. Szymańska, P. Chałupnik, B. Nielsen, D. S. Pickering, T. N. Johansen
    Conference:
    EFMC-ISMC 2018 XXV EFMC International Symposium on Medicinal Chemistry (year: 2018, pages: 341 P416), Publisher: EFMC
    Date:
    conference 2-6.09.
    Status:
    Published

  7. Antagonista receptora AMPA jako nowy, obiecujący, wielofunkcyjny ligand w leczeniu schorzeń neurodegeneracyjnych

    Authors:
    G. Latacz, A. Martyniak, A. Olejarz, E. Szymańska, K. Kieć-Kononowicz
    Conference:
    XXIII Naukowy Zjazd PTFarm - Farmacja w Polsce: perspektywy nauki i zawodu (year: 2017, pages: 120), Publisher: Polskie Towarzystwo Farmaceutyczne
    Date:
    conference 19-22.09
    Status:
    Published

  8. AMPA/KA receptors antagonists with potent antioxidative activity

    Authors:
    G. Latacz, A. Śliwka-Kielar, E. Szymańska, K. Kieć-Kononowicz
    Conference:
    VIII Konwersatorium Chemii Medycznej (year: 2016, pages: P46), Publisher: Polskie Towrarzystwo Chemii Medycznej
    Date:
    conference 15-17.09
    Status:
    Published

  9. Search on phenylalanine-based AMPA receptor ligands

    Authors:
    E. Szymańska, A.M. Cuñado Moral, D.S. Pickering, B. Nielsen, T.N. Johansen, K. Kieć-Kononowicz
    Conference:
    VIII Konwersatorium Chemii Medycznej (year: 2016, pages: P42), Publisher: Polskie Towarzystwo Chemii Medycznej
    Date:
    conference 17-19.09
    Status:
    Published

  10. Search on phenylalanine-based AMPA receptor ligands

    Authors:
    E. Szymańska, T.N. Johansen, B. Nielsen, K. Kieć-Kononowicz
    Conference:
    VII Konwersatorium Chemii Medycznej (year: 2015, pages: P99), Publisher: Polskie Towarzystwo Chemii Medycznej
    Date:
    conference 15-17.09
    Status:
    Published

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