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Search for new "drug-like" molecules designed as adenosine receptors ligands

2012/04/M/NZ4/00219

Keywords

Descriptors

  • ST5_16: Chemia biologiczna
  • NZ4_12: Inne zagadnienia pokrewne
  • NZ1_1: Biologia molekularna

Panel

NZ4 – Biology of tissues, organs and organisms: morphology and functions of animal's and human's systems, organs and organisms, experimental medicine, basics of neurology

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)

prof. Katarzyna Justyna Kieć-Kononowicz

Number of co-investigators in the project: 17

Call

HARMONIA 2 – announced on 2011-12-15

Amount awarded
699 400 PLN
Project start date
2012-09-25
Project end date
2016-09-24
Project duration
48 months (the same as in the proposal)
Project status
Project settled

Information in the final report

Publication in academic press/journals (6)

  1. Evaluation of antidepressant-like and anxiolytic-like activity of purinedione-derivatives with affinity for adenosine A2A receptors in mice

    Authors:
    A. Dziubina, K. Szmyd, M. Zygmunt, J. Sapa, M. Dudek, B. Filipek, A. Drabczynska, M. Załuski, K. Pytka, K. Kiec-Kononowicz
    Academic press:
    Pharmacological Reports (year: 2016, volume: 68, pages: 1285-1292), Publisher: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.pharep.2016.07.008 – link to the publication

  2. Similarities and differences in affinity and binding modes of tricyclic pyrimido- and pyrazinoxanthines at human and rat adenosine receptors

    Authors:
    E. Szymanska, A. Drabczynska, T. Karcz, C.E. Müller, M. Köse, J. Karolak-Wojciechowska, A. Fruzinski, J. Schabikowski, A. Doroz-Płonka, J. Handzlik, K. Kiec-Kononowicz
    Academic press:
    Bioorganic & Medicinal Chemistry (year: 2016, volume: 24, pages: 4347-4362), Publisher: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.bmc.2016.07.028 – link to the publication

  3. Anti-inflammatory, antioxidant and antiparkinsonian effects of adenosine A2A receptor antagonists

    Authors:
    M. Zygmunt, K. Gołembiowska, A. Drabczyńska, K. Kieć-Kononowicz, J. Sapa
    Academic press:
    Pharmacology, Biochemistry and Behaviour (year: 2015, volume: 132, pages: 71-78), Publisher: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.pbb.2015.02.020. – link to the publication

  4. Synthesis, biological activity and molecular modelling studies of tricyclic alkylimidazo-, pyrimido- and diazepinopurinediones

    Authors:
    Anna Drabczyńska; Tadeusz Karcz; Ewa Szymańska; Meryem Köse; Christa E. Müller; Minka Paskaleva; Janina Karolak-Wojciechowska; Jadwiga Handzlik; Olga Yuzlenko; Katarzyna Kieć-Kononowicz
    Academic press:
    Purinergic Signalling (year: 2013, volume: 9, pages: 395–414), Publisher: SpringerLink
    Status:
    Published
    DOI:
    10.1007/s11302-013-9358-3 – link to the publication

  5. Synthesis and analgesic activity of annelated xanthine derivatives in experimental models in rodents

    Authors:
    M.Zygmunt, J.Sapa, A.Drabczyńska, T.Karcz, Ch.Műller, M.Kősse, G.Latacz, J.Schabikowski, M.Bednarski, K.Kieć-Kononowicz
    Academic press:
    Archiv der Pharmazie (year: 2015, volume: 348, pages: 704-714), Publisher: WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
    Status:
    Published
    DOI:
    10.1002/ardp.201500169 – link to the publication

  6. Methods for the synthesis of xanthine-derived polycyclic fused systems

    Authors:
    Ewa Szymańska; Jakub Mazurkiewicz; Katarzyna Kieć-Kononowicz
    Academic press:
    Heterocyclic Communications (year: 2013, volume: 19, pages: 297-310), Publisher: De Gruyter
    Status:
    Published
    DOI:
    10.1515/hc-2013-0082 – link to the publication

Articles in post-conference publications (38)

  1. Anelowane pochodne ksantyn o aktywności hamującej monoaminooksydazę B jako związki o potencjalnym zastosowaniu w chorobach neurodegeneracyjnych

    Authors:
    M. Załuski, J. Schabikowski, T. Karcz, A. Olejarz, A. Doroz-Płonka, K. Kieć-Kononowicz
    Conference:
    VI Konferencja Doktorantów Uniwersytetu Jagiellonskiego Collegium Medicum (year: 2016, pages: 136), Publisher: Towarzystwo Doktorantów UJ
    Date:
    conference 23,04
    Status:
    Published

  2. Comparision of alkyl amide 1,3-dialkilopirymido- and pyrazino [2,1-f]purinedione derivatives in role of adenosine receptor ligands

    Authors:
    J.Mazurkiewicz, M.Załuski, K.Stanuch, T.Karcz, C.E.Muller, K.Kieć-Kononowicz
    Conference:
    7th Summer School Medicinal Chemistry (year: 2014, pages: 118), Publisher: University of Regensburg
    Date:
    conference 17-19.09
    Status:
    Published

  3. Binding mode prediction of tricyclic xanthine derivatives at the orthosteric ligand-binding site of A2A and A2B adenosine receptors

    Authors:
    E.Szymańska, A.Drabczyńska, T.Karcz, C.E.Müller, K.Kieć-Kononowicz
    Conference:
    Glisten Budapest 2014 Conference (year: 2014, pages: 60), Publisher: European Science Foundation COST Action CM1207
    Date:
    conference 2.10-4.10
    Status:
    Published

  4. Annelated xanthines as A1/A2A/A2B adenosine receptors ligands

    Authors:
    A.Drabczyńska, T.Karcz, C.E.Müller, M.Kőse, G.Latacz, J.Mazurkiewicz, M.Załuski, A.Olejarz, J.Handzlik, K.Kieć-Kononowicz
    Conference:
    GLISTEN Budapest 2014 Conference (year: 2014, pages: 25), Publisher: European Science Foundation COST Action CM1207
    Date:
    conference 2.10 – 4.10
    Status:
    Published

  5. Looking for adenosine receptor ligands with drug-like properties

    Authors:
    3)A.Drabczyńska, M.Kőse, C.E.Müller, T.Karcz, E.Szymańska, J.Handzlik, A.Olejarz, J.Mazurkiewicz, G.Latacz, M.Zygmunt, K.Kieć-Kononowicz
    Conference:
    XXIII International Symposium on Medicinal Chemistry (year: 2014, pages: xx), Publisher: European Federation for Medicinal Chemistry (EFMC)
    Date:
    conference 7-11.09
    Status:
    Published

  6. Functional characterization and evaluation of adenosine receptors role in PC-3 cancer cells proliferation

    Authors:
    A.Olejarz, T.Karcz, K.Kieć-Kononowicz
    Conference:
    4th Meeting of the Paul Ehrlich MedChem Euro-PhD Network (year: 2014, pages: 61), Publisher: CHARLES UNIVERSITY IN PRAGUE FACULTY OF PHARMACY IN HRADEC KRÁLOVÉ
    Date:
    conference 20-22.06
    Status:
    Published

  7. Alkyl- and cyclo-alkylamide substituted derivatives of 1,3-dialkylpyrimido[2,1-f]purinediones as ligands of the adenosine receptors

    Authors:
    M.Załuski, K.Stanuch, T.Karcz, C.E.Müller, M.Kőse, K.Kieć-Konnowicz
    Conference:
    VI Konwersatorium Chemii Medycznej (year: 2014, pages: 203), Publisher: Polskie Towarzystwo Chemii Medycznej
    Date:
    conference 18-21.09
    Status:
    Published

  8. Comparison of 1,3-dimethyl-pyrimido- and pyrazino[2,1-f]purinediones substituted via an ether linker as adenosine receptor antagonists

    Authors:
    J.Mazurkiewicz, A.Drabczyńska, T.Karcz, C.E.Muller, K.Kieć-Kononowicz
    Conference:
    GLISTEN Cost CM1207 – Adenosine receptors: present and future challenges (year: 2015, pages: Poster 16), Publisher: European Science Foundation COST Action CM1207
    Date:
    conference 2.03 - 3.03
    Status:
    Published

  9. Poszukiwania ligandów receptorów adenozynowych wśród pochodnych 1,3-dialkilopirymido- oraz pirazyno[2,1-f]purynodionów

    Authors:
    J.Schabikowski, M.Załuski, A.Drabczyńska, K.Stanuch, T.Karcz, C.E.Muller, K.Kieć-Kononowicz
    Conference:
    V Konferencja Doktorantów Collegium Medicum UJ (year: 2015, pages: 130), Publisher: Towarzystwo Doktorantów UJ
    Date:
    conference 28.05 - 29.05
    Status:
    Published

  10. Wstępna ocena bezpieczeństwa metodami in vitro nowych, silnych i selektywnych ligandów receptora adenozynowego

    Authors:
    A.Lubelska, K.Pawlak, K.Witek, G.Latacz, J.Handzlik, K.Kieć-Kononowicz
    Conference:
    V Konferencja Doktorantów Collegium Medicum UJ (year: 2015, pages: 84), Publisher: Towarzystwo Doktorantów UJ
    Date:
    conference 28.05 - 29.05
    Status:
    Published

  11. Adenosine receptor ligands with potent antioxidantive activity

    Authors:
    G.Latacz, A.Drabczyńska, A.Sala, C.E.Muller, K.Kieć-Kononowicz
    Conference:
    GLISTEN Cost CM1207 – Adenosine receptors: present and future challenges (year: 2015, pages: Poster 6), Publisher: European Science Foundation COST Action CM1207
    Date:
    conference 2.03 - 3.03
    Status:
    Published

  12. Amide-substituted 1,3-dialkylpyrimido[2,1-f]purinediones as adenosine receptor antagonists

    Authors:
    M.Załuski, A.Drabczyńska, K.Stanuch T.Karcz, C.E.Muller, K.Kieć-Kononowicz
    Conference:
    GLISTEN Cost CM1207 – Adenosine receptors: prezent and future challenges (year: 2015, pages: Poster 14), Publisher: European Science Foundation COST Action CM1207
    Date:
    conference 2.03 - 3.03
    Status:
    Published

  13. Phenol derivatives of 1,3-dialkyl-pyrimido[2,1-f]purinediones, evaluation of intrinsic activity and interspecies affinity differences at adenosine receptors subtypes

    Authors:
    T.Karcz, A.Drabczyńska, C,E.Muller, K.Kieć-Kononowicz
    Conference:
    GLISTEN Cost CM1207 – Adenosine receptors: present and future challenges (year: 2015, pages: Poster 15), Publisher: European Science Foundation COST Action CM1207
    Date:
    conference 2.03 - 3.03
    Status:
    Published

  14. Analgesic activity of tricyclic annelated derivatives of xanthenes with affinity at adenosine receptors

    Authors:
    M.Zygmunt, T.Karcz, C.E.Müller, B.Filipek, K.Kieć-Kononowicz
    Conference:
    Vth Conversatory on Medicinal Chemistry (year: 2012, pages: P-26), Publisher: Chair and Department of Synthesis and Chemical Technology of Pharmaceutical Substances, Faculty of Pharmacy, Medical University of Lublin
    Date:
    conference 13.09-15.09.2012
    Status:
    Published

  15. Search for adenosine receptors ligands among annelated xanthine derivatives

    Authors:
    A.Drabczyńska, T.Karcz, E.Szymańska, C.Müller, M.Kőse, M.Zygmunt, J.Sapa, G.Latacz, J.Mazurkiewicz, K.Stanuch, M.Załuski, A.Olejarz, K.Kieć-Kononowicz
    Conference:
    Purines in Bonn - Nucleotides, Nocleosides and Nucleobases (year: 2014, pages: 41), Publisher: Uniwersytet w Bonn
    Date:
    conference 23-27.07
    Status:
    Published

  16. Drug-likeness properties of the most active A1/A2A adenosine receptor ligands among N-substituted tricyclic xanthine derivatives

    Authors:
    A.Drabczyńska, J.Handzlik, M.Kőse, T.Karcz, C.E.Müller, G.Latacz, K.Kieć-Kononowicz
    Conference:
    Purines in Bonn - Nucleotides, Nocleosides and Nucleobases (year: 2014, pages: 189), Publisher: Uniwersytet w Bonn
    Date:
    conference 23-27.07
    Status:
    Published

  17. Searching for antiparkinsonian drugs considering dopamine and adenosine A2A receptor ligands

    Authors:
    K.Kieć-Kononowicz, A. Drabczyńska, T. Karcz, C. E. Müller:, M. Zygmunt, J. Sapa
    Conference:
    Meeting of the Polish Histamine Research Society & COST Action CM 1103 (year: 2012, pages: 28), Publisher: Polish Histamine Research Society
    Date:
    conference 25-27.10.2012
    Status:
    Published

  18. Binding mode prediction of tricyclic xanthine derivatives as antagonists of adenosine receptors

    Authors:
    E.Szymańska, A.Drabczyńska, T.Karcz, C.E.Müller, M.Paskaleva, K.Kieć-Kononowicz
    Conference:
    VIIIth Joint Meeting on Medicinal Chemistry (year: 2013, pages: KN-I), Publisher: Chair and Department of Synthesis and Chemical Technology of Pharmaceutical Substances, Faculty of Pharmacy, Medical University of Lublin
    Date:
    conference 30.06-4.07.2013
    Status:
    Published

  19. Search for new ligands of A2B adenosine receptors in the group of 1,3-dialkylpyrimido[2,1-f]-purinediones

    Authors:
    A.Drabczyńska, T.Karcz, C.E.Müller, J.Handzlik, K.Kieć-Kononowicz
    Conference:
    22 Naukowy Zjazd PTFarm (year: 2013, pages: 317), Publisher: Polskie Towarzystwo Farmaceutyczne
    Date:
    conference 18-21.09.2013
    Status:
    Published

  20. N-9 aryloalkilowe pochodne 1,3-dimetylpirymido[2,1-f]purynodionów o aktywności hamującej monoaminooksydazę B jako związki o potencjalnym zastosowaniu w chorobach neurodegeneracyjnych

    Authors:
    M.Załuski, A.Olejarz, T.Karcz, Ch.Müller, K.Kieć-Kononowicz
    Conference:
    V Konferencja Doktorantów Collegium Medicum UJ (year: 2015, pages: 168-169), Publisher: Towarzystwo Doktorantów UJ
    Date:
    conference 28.05 - 29.05
    Status:
    Published

  21. Multi-targeting xanthine derivatives

    Authors:
    T. Karcz, A.Drabczyńska, A. Olejarz, M. Kose, S. Hinz, C.E. Muller, K.Kieć-Kononowicz
    Conference:
    Frontiers in Medicinal Chemistry (year: 2016, pages: 133), Publisher: Gesellschaft Deutscher Chemiker
    Date:
    conference 13-16.03
    Status:
    Published

  22. Influence of tricyclic xanthine derivatives on activity of monoamine oxidase B

    Authors:
    U. Cichon, A. Olejarz, M. Hagan, A.Drabczyńska, J. Schabikowski, M. Zaluski, T. Karcz, K.Kieć-Kononowicz
    Conference:
    VIII Konwersatorium Chemii Medycznej (year: 2016, pages: P-102), Publisher: Polskie Towarzystwo Chemii Medycznej
    Date:
    conference 15-17.09
    Status:
    Published

  23. Similarities and differences in affinity and binding modes of tricyclic pyrimidoxanthines at human and rat adenosine receptors

    Authors:
    E. Szymanska, A.Drabczyńska, T. Karcz, C.E. Muller, K.Kieć-Kononowicz
    Conference:
    Glisten in Prague (year: 2016, pages: 65), Publisher: University of Chemistry and Technology in Prague
    Date:
    conference 25-27.09
    Status:
    Published

  24. Looking for multi-target acting xanthine derivatives

    Authors:
    T.Karcz, A.Drabczyńska, A.Olejarz, M.Kőse, S.Hinz, A.Doroz-Płonka, B.Kubas, C.E.Müller, K.Kieć-Kononowicz
    Conference:
    DPh Jahrestagung 2015, Annual Meeting (year: 2015, pages: 174), Publisher: Deutsche Pharmazeutische Gesellschaft e.V.
    Date:
    conference 23.09 - 25.09
    Status:
    Published

  25. A homogenous A2B adenosine receptor fluorescence binding assay based on flow cytometry

    Authors:
    M.Kőse, T.Karcz, S.Gollos, A.Fiene, F.Heisig, C.Spanier, K.Kieć-Kononowicz, C.E.Müller
    Conference:
    DPh Jahrestagung 2015, Annual Meeting (year: 2015, pages: 146), Publisher: Deutsche Pharmazeutische Gesellschaft e.V.
    Date:
    conference 23.09 - 25.09
    Status:
    Published

  26. Development of dual target adenosine A1/A2A receptors antagonists among annelated xanthine derivatives

    Authors:
    J. Schabikowski, M. Zaluski, T. Karcz, S. Hinz, E. Szymanska, J. Handzlik, C.E. Muller, K.Kieć-Kononowicz
    Conference:
    First Annual Meeting COST Action CA15135 (year: 2016, pages: 23), Publisher: Universita della Svizzera Italiana USI
    Date:
    conference 21-22.07
    Status:
    Published

  27. Benzylowe pochodne 1-etyloteobrominy jako inhibitory monoaminooksydazy B

    Authors:
    J. Schabikowski, T. Karcz, D. Schabikowska, M. Zaluski, A. Olejarz, A. Doroz-Plonka, K.Kieć-Kononowicz
    Conference:
    VI Konferencja Doktorantów Uniwersytetu Jagiellonskiego Collegium Medicum (year: 2016, pages: 111), Publisher: Towarzystwo Doktorantów UJ
    Date:
    conference 23,04
    Status:
    Published

  28. Monoamine oxidase B activity of novel tricyclic xanthine derivatives

    Authors:
    A. Olejarz, U. Cichon, A.Drabczyńska, J. Schabikowski, M. Zaluski, M. Hagan, T. Karcz, K.Kieć-Kononowicz
    Conference:
    VIII Konwersatorium Chemii Medycznej (year: 2016, pages: P-8), Publisher: Polskie Towarzystwo Chemii Medycznej
    Date:
    conference 15-17.09
    Status:
    Published

  29. N9-benzyl derivatives of pyrimido[2,1-f]purinediones as A1/A2A adenosine receptor ligands and MAO-B inhibitors

    Authors:
    M. Zaluski, B. Kubas, A. Olejarz, T. Karcz, C.E. Muller, K.Kieć-Kononowicz
    Conference:
    VIII Konwersatorium Chemii Medycznej (year: 2016, pages: P-84), Publisher: Polskie Towarzystwo Chemii Medycznej
    Date:
    conference 15-17.09
    Status:
    Published

  30. The evaluation of the antioxidant activity of xanthine derivatives and preliminary study on the neuroprotection against 6-hydroxydopamine neurotoxicity

    Authors:
    B. Zekolli, G. Latacz, J. Aspden, A.Drabczyńska, K.Kieć-Kononowicz
    Conference:
    VIII Konwersatorium Chemii Medycznej (year: 2016, pages: P-27), Publisher: Polskie Towarzystwo Chemii Medycznej
    Date:
    conference 15-17.09
    Status:
    Published

  31. Tricyclic xanthine derivatives as MAO-B inhibitors

    Authors:
    J.Schabikowski, T.Karcz, M.Załuski, B.Kubas, A.Doroz-Płonka, K.Kieć-Kononowicz
    Conference:
    VII Konwersatorium Chemii Medycznej (year: 2015, pages: P89), Publisher: Polskie Towarzystwo Chemii Medycznej
    Date:
    conference 17.09 - 20.09
    Status:
    Published

  32. Comparison of 1,3-dialkyl-pyrimido- and pyrazino[2,1-f]purinediones containing alkylamide moieties as adenosine receptor antagonists

    Authors:
    J.Schabikowski, M.Załuski, A.Drabczyńska, T.Karcz, Ch.Müller, K.Kieć-Kononowicz
    Conference:
    6th Joint German-Italian Purine Club Meeting, International Conference on Purinergic Signalling (year: 2015, pages: 78-79), Publisher: German-Italian Purine Club
    Date:
    conference 23.07 – 25.07
    Status:
    Published

  33. Amide substituted 1,3-dipropylpyrimido [2,1-f]purinediones as antagonists of the adenosine receptors

    Authors:
    M.Załuski, T.Karcz, Ch.Müller, K.Kieć-Kononowicz
    Conference:
    V Meeting of the Paul Ehrlich MedChem Euro-PhD Network (year: 2015, pages: 35), Publisher: Paul Ehrlich MedChem Euro-PhD Network
    Date:
    conference 3.07 - 5.07
    Status:
    Published

  34. Phenol substituted derivatives of 1,3-dimethylpyrazino-(2,1-f)-purinediones as the adenosine receptor ligands

    Authors:
    J.Schabikowski, T.Karcz, CH.Műller, K.Kieć-Kononowicz
    Conference:
    V Meeting of the Paul Ehrlich MedChem Euro-PhD Network (year: 2015, pages: 90), Publisher: Paul Ehrlich MedChem Euro-PhD Network
    Date:
    conference 3.07 - 5.07
    Status:
    Published

  35. Evaluation of novel 1,3-dialkyllpyrimido[2,1-f]purinediones as adenosine receptor antagonists

    Authors:
    M.Załuski, A.Drabczyńska, Ch.Müller, T.Karcz, J.Schabikowski, K.Stanuch, K.Kieć-Kononowicz
    Conference:
    6th Joint German-Italian Purine Club Meeting, International Conference on Purinergic Signalling (year: 2015, pages: 81-82), Publisher: German-Italian Purine Club
    Date:
    conference 23 – 25.07
    Status:
    Published

  36. Evaluation of novel N-9-benzyl-disubstituted derivatives of 1,3-dimethylpyrimido[2,1-f]purinediones as MAO-B inhibitors

    Authors:
    M.Załuski, B.Kubas, A.Olejarz, T.Karcz, K.Kieć-Kononowicz
    Conference:
    VII Konwersatorium Chemii Medycznej (year: 2015, pages: PP14), Publisher: Polskie Towarzystwo Chemii Medycznej
    Date:
    conference 17.09 - 20.09
    Status:
    Published

  37. Porównanie alkiloamidowych pochodnych 1,3-dialkilopirymido- i pirazyno[2,1-f]purynodionów jako ligandów receptorów adenozynowych

    Authors:
    J.Mazurkiewicz, M.Załuski, K.Stanuch, T.Karcz, C.E.Müller, K.Kieć-Kononowicz
    Conference:
    Konferencja Doktorantów CM UJ (year: 2014, pages: 139-140), Publisher: Towarzystwo Doktorantów CM UJ
    Date:
    conference 29.05-30.05
    Status:
    Published

  38. Porównanie alkiloamidowych pochodnych 1,3-dialkilopirymido- i pirazyno[2,1-f]purynodionów jako ligandów receptorów adenozynowych

    Authors:
    J.Schabikowski, M.Załuski, A.Drabczyńska, T.Karcz, C.Müller, K.Karcz, K.Kieć-Kononowicz
    Conference:
    I Ogólnopolska Konferencja Młodych Naukowców AZYMUT (year: 2015, pages: 116), Publisher: Politechnika Warszawska Towarzystwo Młodzi Naukowcy AZYMUT
    Date:
    conference 17,06
    Status:
    Published

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