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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Amine derivatives of hydantoin as selective 5-HT7 receptor ligand. Molecular modeling, synthesis and pharmacological evaluation.

2014/15/N/NZ7/03072

Keywords:

5-HT7 hydantoins selectivity

Descriptors:

  • NZ7_14: Pharmacy, pharmacotherapy, pharmacology
  • ST5_16:
  • NZ2_7: Bioinformatics

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 Uniwersytet Jagielloński, Wydział Farmaceutyczny

woj. małopolskie

Other projects carried out by the institution 

Principal investigator (from the host institution):

Katarzyna Kucwaj-Brysz 

Number of co-investigators in the project: 2

Call: PRELUDIUM 8 - announced on 2014-09-15

Amount awarded: 96 562 PLN

Project start date (Y-m-d): 2015-09-21

Project end date (Y-m-d): 2018-03-20

Project duration:: 30 months (the same as in the proposal)

Project status: Project settled

Equipment purchased [PL]

  1. Wyparka próżniowa z zaworem i weżem do próżni (20 295 PLN)
  2. Laptop z oprogramowaniem do modelowania molekularnego (Schrodinger) (18 000 PLN)
  3. Mieszadło magnetyczne z termometrem kontaktowym (2 435 PLN)

Information in the final report

  • Publication in academic press/journals (5)
  1. In the search for a lead structure among series of potent and selective hydantoin 5‐HT7R agents: The drug‐likeness in vitro study
    Authors:
    Gniewomir Latacz, Annamaria Lubelska, Magdalena Jastrzębska-Więsek, Anna Partyka, Andrzej Sobiło, Agnieszka Olejarz, Katarzyna Kucwaj-Brysz, Grzegorz Satała, Andrzej J. Bojarski, Anna Wesołowska, Katarzyna Kieć-Kononowicz, Jadwiga Handzlik
    Academic press:
    Chemical Biology and Drug Design (rok: 2017, tom: 90, strony: 1295-1306), Wydawca: Wiley
    Status:
    Published
    DOI:
    10.1111/cbdd.13106 - link to the publication
  2. MF-8, a novel promising arylpiperazine-hydantoin based 5-HT7 receptor antagonist: In vitro drug-likeness studies and in vivo pharmacological evaluation
    Authors:
    Gniewomir Latacz, Annamaria Lubelska, MagdalenaJastrzębska-Więsek, Anna Partyka, Katarzyna Kucwaj-Brysz, Anna Wesołowska, Katarzyna Kieć-Kononowicz, Jadwiga Handzlik
    Academic press:
    Bioorganic and Medicinal Chemistry Letters (rok: 2018, tom: 28, strony: 878-883), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.bmcl.2018.02.003 - link to the publication
  3. Rational design in search for 5-phenylhydantoin selective 5-HT7R antagonists. Molecular modeling, synthesis and biological evaluation
    Authors:
    Katarzyna Kucwaj-Brysz, Dawid Warszycki, Sabina Podlewska, Jagna Witek, Karolina Witek, Andrea González Izquierdo, Grzegorz Satała, María I. Loza, Annamaria Lubelska, Gniewomir Latacz, Andrzej J. Bojarski, Marián Castro, Katarzyna Kieć-Kononowicz, Jadwiga Handzlik
    Academic press:
    European Journal of Medicinal Chemistry (rok: 2016, tom: 112, strony: 258-269), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2016.02.024 - link to the publication
  4. The role of aryl-topology in balancing between selective and dual 5-HT7R/5-HT1A actions of 3,5-substituted hydantoins
    Authors:
    Katarzyna Kucwaj-Brysz, Rafał Kurczab, Ewa Żesławska, Annamaria Lubelska, Małgorzata Anna Marć, Gniewomir Latacz, Grzegorz Satała, Wojciech Nitek, Katarzyna Kieć-Kononowicz, Jadwiga Handzlik
    Academic press:
    MedChemComm (rok: 2018, tom: 9, strony: 1033-1044), Wydawca: Royal Society of Chemistry
    Status:
    Published
    DOI:
    10.1039/C8MD00168E - link to the publication
  5. Computer-aided insights into receptor-ligand interaction for novel 5-arylhydantoin derivatives as serotonin 5-HT7 receptor agents with antidepressant activity
    Authors:
    Katarzyna Kucwaj-Brysz, Rafał Kurczab, Magdalena Jastrzębska-Więsek, Ewa Żesławska, Grzegorz Satała, Wojciech Nitek, Anna Partyka, Agata Siwek, Agnieszka Jankowska, Anna Wesołowska, Katarzyna Kieć-Kononowicz, Jadwiga Handzlik
    Academic press:
    European Journal of Medicinal Chemistry (rok: 2018, tom: 147, strony: 102-114), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2018.01.093 - link to the publication