Amine derivatives of hydantoin as selective 5-HT7 receptor ligand. Molecular modeling, synthesis and pharmacological evaluation.
2014/15/N/NZ7/03072
Keywords
Descriptors
- NZ7_14: Farmacja, farmakoterapia, farmakologia
- ST5_16: Chemia biologiczna
- NZ2_7: Bioinformatyka
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
Voivodeship: małopolskie
Principal investigator (from the host institution)
Number of co-investigators in the project: 2
Call
PRELUDIUM 8 – announced on 2014-09-15
- Amount awarded
- 96 562 PLN
- Project start date
- 2015-09-21
- Project end date
- 2018-03-20
- Project duration
- 30 months (the same as in the proposal)
- Project status
- Project settled
Equipment purchased [PL]
- Laptop z oprogramowaniem do modelowania molekularnego (Schrodinger). Cost: 18 000 PLN
- Mieszadło magnetyczne z termometrem kontaktowym. Cost: 2 435 PLN
- Wyparka próżniowa z zaworem i weżem do próżni. Cost: 20 295 PLN
Information in the final report
Publication in academic press/journals (5)
-
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 (year: 2016, volume: 112, pages: 258-269), Publisher: Elsevier
- Status:
- Published
- DOI:
- 10.1016/j.ejmech.2016.02.024 – link to the publication
-
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 (year: 2017, volume: 90, pages: 1295-1306), Publisher: Wiley
- Status:
- Published
- DOI:
- 10.1111/cbdd.13106 – link to the publication
-
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 (year: 2018, volume: 9, pages: 1033-1044), Publisher: Royal Society of Chemistry
- Status:
- Published
- DOI:
- 10.1039/C8MD00168E – link to the publication
-
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 (year: 2018, volume: 28, pages: 878-883), Publisher: Elsevier
- Status:
- Published
- DOI:
- 10.1016/j.bmcl.2018.02.003 – link to the publication
-
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 (year: 2018, volume: 147, pages: 102-114), Publisher: Elsevier
- Status:
- Published
- DOI:
- 10.1016/j.ejmech.2018.01.093 – link to the publication