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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Synthesis, physicochemical and pharmacological properties of new amide derivatives of 3,3-disubstituted pyrrolidine-2,5-dione-alkyl acids with potential activity on central nervous system

2013/11/B/NZ7/02081

Keywords:

pyrrolidine-2,5-diones piperazinamides anticonvulsant antidepressant activity neuropatic pain

Descriptors:

  • NZ7_14: Pharmacy, pharmacotherapy, pharmacology
  • ST5_16:
  • ST5_23:

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):

prof. Jolanta Obniska 

Number of co-investigators in the project: 6

Call: OPUS 6 - announced on 2013-09-16

Amount awarded: 396 600 PLN

Project start date (Y-m-d): 2014-08-21

Project end date (Y-m-d): 2017-08-20

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

Project status: Project settled

Equipment purchased [PL]

  1. komputer stacjonarny (1 656 PLN)
  2. Stymulator z elektrodami do testu 6-Hz (24 000 PLN)
  3. Lampa UV (6 000 PLN)

Information in the final report

  • Publication in academic press/journals (5)
  • Articles in post-conference publications (9)
  1. Design, synthesis and biological activity of new amides derived from 3-methyl-3-phenyl-2,5-dioxo-pyrrolidin-1-yl-acetic acid
    Authors:
    J. Obniska, A. Rapacz, S. Rybka, B. Powroźnik, E. Pękala, B. Filipek, P. Żmudzki, K. Kamiński
    Academic press:
    Eur. J. Med. Chem. (rok: 2015, tom: 102, strony: 14-25), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/ejmech.2015.07.017 - link to the publication
  2. Synthesis and anticonvulsant properties of new 3,3-diphenyl-2,5-dioxo-pyrrolidin-1-yl-acetamides and 3,3-diphenyl-propionamides
    Authors:
    J.Obniska, A.Rapacz, S. Rybka, M. Góra, P. Zmudzki, K. Kamiński
    Academic press:
    Arch. Pharm.Chem.Life Sci. (rok: 2017, tom: 350, strony: 45305), Wydawca: Welly
    Status:
    Published
    DOI:
    10.1002/ardp.201600368 - link to the publication
  3. Antiallodynic and antihyperalgesic activity of new 3,3-diphenylpropionamides with anticonvulsant activity in models of pain in mice
    Authors:
    A. Rapacz, J. Obniska, P. Koczurkiewicz, K. Wójcik Pszczoła, A. Siwek, A. Gryboś, S. Rybka, A. Karcz, E. Pękala. B. Filipek
    Academic press:
    Eur. J. Pharmacol. (rok: 2018, tom: 821, strony: 39-48), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejphar.2017.12.036 - link to the publication
  4. Anticonvulsant and antinociceptive activity of new amides derived from 3-phenyl-2,5-dioxo-pyrrolidine-1-yl-acetic acid in mice
    Authors:
    A. Rapacz, J. Obniska, B. Wiklik-Poudel, S. Rybka, K. Sałat, B. Filipek
    Academic press:
    Eur J Pharmacol (rok: 2016, tom: 781, strony: 239-249), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejphar.2016.04.033 - link to the publication
  5. Synthesis, and anticonvulsant activity of new amides derived from 3-methyl- or 3-ethyl-3-methyl-2,5-dioxo-pyrrolidin-1-yl-acetic acids
    Authors:
    J. Obniska, A. Rapacz, S. Rybka, M. Góra, K. Kamiński, K. Sałat, P. Żmudzki
    Academic press:
    Bioorg Med Chem (rok: 2016, tom: 24, strony: 1598-1607), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.bmc.2016.02.026 - link to the publication
  1. Analgesic and antiallodynic properties of new 3,3-diphenyl-propionamides with anticonvulsant activity
    Authors:
    A. Rapacz, J. Obniska
    Conference:
    13th International Congress Polish Neuroscience Society (rok: 2017, ), Wydawca: Acta Neurobiologiae Experimentalis
    Data:
    konferencja 28-31 sierpień
    Status:
    Published
  2. Design, synthesis, physicochemical and anticonvulsant properties of new amides derived from 3-methyl-3-phenyl-2,5-dioxo-pyrrolidin-1-ylpropionic and 3-phenyl-butanoic acid
    Authors:
    J. Obniska, S. Rybka, A. Rapacz, A. Chudzińska, K. Kamiński
    Conference:
    17th Tetrahedron Symposium (rok: 2016, ), Wydawca: Elsevier
    Data:
    konferencja 28.06-1.07
    Status:
    Published
  3. Synthesis of new piperazinamides derived from 3-(1-phenylethyl)-2,5-dioxo-pyrrolidin-1-yl-acetic acid with potential anticonvulsant activity
    Authors:
    J. Obniska, A. Rapacz, K. Kamiński, M. Góra
    Conference:
    17th Hellenic Symposium on Medicinal Chemistry: Designing targeted and safer drugs (rok: 2017, ), Wydawca: Hellenic Society of Medicinal Chemistry (Greece)
    Data:
    konferencja 1-3.06 Saloniki
    Status:
    Published
  4. Design, synthesis and anticonvulsant activity of new piperazinamides derived from 3-isobutyl-2,5-dioxopyrrolidin-1-yl-acetic acid
    Authors:
    J. Obniska, M. Góra, S. Rybka, K. Kamiński, A. Rapacz
    Conference:
    10th Joint Meeting on Medicinal Chemistry (rok: 2017, ), Wydawca: EFMC
    Data:
    konferencja 25-28 .06
    Status:
    Published
  5. Design, synthesis of new amides derived from 3,3-disubstituted 2,5-dioxo-pyrrolidin-1-yl-acetic acid as potential anticonvulsant agents
    Authors:
    J. Obniska, S. Rybka, A. Rapacz, K. Kamiński, M. Góra
    Conference:
    Drug Discovery and Selection - RICT 2o15 (rok: 2015, ), Wydawca: Societe de Chimie Therapeutique
    Data:
    konferencja 1-3 July
    Status:
    Published
  6. Synthesis and evaluation of anticonvulsant properties of new amides derived from 3,3-diphenyl-2,5-dioxo-pyrrolidine-1-yl-acetic acid
    Authors:
    J. Obniska, A. Rapacz, S. Rybka, K. Kamiński, M. Góra
    Conference:
    VIII Konwersatorium Chemii Medycznej (rok: 2016, ), Wydawca: Polskie Towarzystwo Chemii Medycznej
    Data:
    konferencja 15-17 września
    Status:
    Published
  7. Synthesis,physicochemical properties of new piperazinamides of aryl-alkyl acids with potential anticonvulsant activity
    Authors:
    J. Obniska, A. Rapacz, S. Rybka, K. Kamiński, A. Chudzińska, M. Góra
    Conference:
    VII Konwersatorium Chemii Medycznej & VIII Sympozjum PTBI (rok: 2015, ), Wydawca: Polskie Towarzystwo Chemii Medycznej
    Data:
    konferencja 17-19 wrzesień Lublin
    Status:
    Published
  8. Aktywność przeciwbólowa nowych amidowych pochodnych 3-fenylo-3-metylopirolidyno-2,5-dionu w modelu bólu neuropatycznego indukowanego podaniem oksaliplatyny u myszy
    Authors:
    A. Rapacz, K. Sałat, B. Filipek, A. Furgała, S. Rybka, J. Obniska
    Conference:
    XXXI Ogólnopolskie seminarium Mechanizmy służące utrzymaniu życia i regulacji fizjologicznych" (rok: 2017, ), Wydawca: Małopolska Wyższa Szkoła im. Józefa Dietla w Krakowie
    Data:
    konferencja 24 czerwiec
    Status:
    Published
  9. Antinociceptive activity of new amides derived from 3-phenyl-2,5-dioxo-pyrrolidine-1-yl-acetic acid in pain models in mice.
    Authors:
    A. Rapacz, A. Furgała, K. Grabczak, S. Rybka, B. Wiklik-Poudel, J. Obniska, B. Filipek, K. Sałat
    Conference:
    XXIV International Symposium "Molecular and Physiological Aspects of Regulatory Process of the Organism" (rok: 2015, ), Wydawca: Joseph Dietl Malopolska Higher School in Cracow
    Data:
    konferencja 26 wrzesień
    Status:
    Published