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New perspective in Alzheimer's disease therapy - multifunctional histamine H3 receptor ligands?

2016/23/B/NZ7/02327

Keywords

Descriptors

  • NZ7_4: Prewencja populacyjna
  • NZ7_14: Farmacja, farmakoterapia, farmakologia
  • ST5_16: Chemia biologiczna

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 hab. Dorota Łażewska

Number of co-investigators in the project: 8

Call

OPUS 12 – announced on 2016-09-15

Amount awarded
791 900 PLN
Project start date
2017-07-25
Project end date
2022-01-24
Project duration
54 months (the same as in the proposal)
Project status
Project settled

Project description

Download the project description in a pdf file

Note — project descriptions were prepared by the authors of the applications themselves and placed in the system in an unchanged form.

Equipment purchased [PL]

  1. Kriostat. Cost: 60 000 PLN
  2. Laptop z moniotem i oprogramowaniem. Cost: 7 000 PLN
  3. Lodówka laboratoryjna. Cost: 18 000 PLN
  4. Pakiet MOE - specjalistyczne oprogramowanie do modelowania molekularnego. Cost: 30 000 PLN
  5. Profesjonalny aparat do mierzenia temperatury topnienia i wrzenia. Cost: 55 000 PLN
  6. Program ACD/Spectrus Processor.
  7. Program EndNote 18(X8) (or nowsza wersja) dla 4-5 użytkowników (5 pcs). Cost: 7 000 PLN
  8. laptop z wyposażeniem.
  9. mieszadło magentyczne z wyposażeniem. Cost: 4 379 PLN
  10. wyparka laboratoryjna z wyposażeniem.

Information in the final report

Publication in academic press/journals (9)

  1. Biphenylalkoxyamine Derivatives-Histamine H3 Receptor Ligands with Butyrylcholinesterase Inhibitory Activity.

    Authors:
    Łażewska D, Zaręba P, Godyń J, Doroz-Płonka A, Frank A, Reiner-Link D, Bajda M, Stary D, Mogilski S, Olejarz-Maciej A, Kaleta M, Stark H, Malawska B, Kieć-Kononowicz K.
    Academic press:
    Molecules (year: 2021, volume: 26, pages: 3580), Publisher: MDPI
    Status:
    Published
    DOI:
    10.3390/molecules26123580 – link to the publication

  2. Rational design of new multitarget histamine H3 receptor ligands as potential candidates for treatment of Alzheimer's disease.

    Authors:
    Łażewska D, Bajda M, Kaleta M, Zaręba P, Doroz-Płonka A, Siwek A, Alachkar A, Mogilski S, Saad A, Kuder K, Olejarz-Maciej A, Godyń J, Stary D, Sudoł S, Więcek M, Latacz G, Walczak M, Handzlik J, Sadek B, Malawska B, Kieć-Kononowicz K.
    Academic press:
    European Journal of Medicinal Chemistry (year: 2020, volume: 207, pages: 112743), Publisher: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2020.112743 – link to the publication

  3. Cyanobiphenyls: Novel H3 receptor ligands with cholinesterase and MAO B inhibitory activity as multitarget compounds for potential treatment of Alzheimer's disease.

    Authors:
    Godyń J, Zaręba P, Łażewska D, Stary D, Reiner-Link D, Frank A, Latacz G, Mogilski S, Kaleta M, Doroz-Płonka A, Lubelska A, Honkisz-Orzechowska E, Olejarz-Maciej A, Handzlik J, Stark H, Kieć-Kononowicz K, Malawska B, Bajda M.
    Academic press:
    Bioorganic Chemistry (year: 2021, volume: 114, pages: 105129), Publisher: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.bioorg.2021.105129 – link to the publication

  4. Studies on Anticonvulsant Effects of Novel Histamine H3R Antagonists in Electrically and Chemically Induced Seizures in Rats

    Authors:
    Alachkar A, Łażewska D, Latacz G, Frank A, Siwek A, Lubelska A, Honkisz-Orzechowska E, Handzlik J, Stark H, Kieć-Kononowicz K, Sadek B
    Academic press:
    Int J Mol Sci (year: 2018, volume: 19, pages: 3386), Publisher: MDPI
    Status:
    Published
    DOI:
    10.3390/ijms19113386 – link to the publication

  5. 4-tert-Pentylphenoxyalkyl derivatives - Histamine H3 receptor ligands and monoamine oxidase B inhibitors

    Authors:
    Łażewska D, Olejarz-Maciej A, Kaleta M, Bajda M, Siwek A, Karcz T, Doroz-Płonka A, Cichoń U, Kuder K, Kieć-Kononowicz K.
    Academic press:
    Bioorg Med Chem Lett (year: 2018, volume: 28, pages: 3596-3600), Publisher: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.bmcl.2018.10.048 – link to the publication

  6. In silico and in vitro studies on interaction of novel non-imidazole histamine H3R antagonists with CYP3A4.

    Authors:
    Podlewska S, Latacz G, Łażewska D, Kieć-Kononowicz K, Handzlik J.
    Academic press:
    Bioorganic Medicinal Chemistry Letters (year: 2020, volume: 30, pages: 127147), Publisher: Science Direct
    Status:
    Published
    DOI:
    10.1016/j.bmcl.2020.127147 – link to the publication

  7. Search for new multi-target compounds against Alzheimer's disease among histamine H 3 receptor ligands

    Authors:
    Bajda M, Łażewska D, Godyń J, Zaręba P, Kuder K, Hagenow S, Łątka K, Stawarska E, Stark H, Kieć-Kononowicz K, Malawska B.
    Academic press:
    European Journal of Medicinal Chemistry (year: 2020, volume: 185, pages: 111785), Publisher: Science Direct
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2019.111785 – link to the publication

  8. Dual Target Ligands with 4-tert-Butylphenoxy Scaffold as Histamine H3 Receptor Antagonists and Monoamine Oxidase B Inhibitors.

    Authors:
    Łażewska D, Olejarz-Maciej A, Reiner D, Kaleta M, Latacz G, Zygmunt M, Doroz-Płonka A, Karcz T, Frank A, Stark H, Kieć-Kononowicz K.
    Academic press:
    International Journal of Molecular Science (year: 2020, volume: 21, pages: 3411), Publisher: MDPI
    Status:
    Published
    DOI:
    10.3390/ijms21103411 – link to the publication

  9. Progress in the development of histamine H3 receptor antagonists/inverse agonists: a patent review (2013-2017)

    Authors:
    Łażewska D, Kieć-Kononowicz K
    Academic press:
    Expert Opin. Ther. Patents (year: 2018, volume: 28, pages: 175-196), Publisher: Taylor&Trancis Group
    Status:
    Published
    DOI:
    10.1080/13543776.2018.1424135 – link to the publication

Articles in post-conference publications (13)

  1. XANTHONE DERIVATIVES AS HISTAMINE H3 RECEPTOR LIGANDS AND CHOLINESTERASE INHIBITORS

    Authors:
    Dorota Łażewska, Marek Bajda, Paula Zaręba, Agata Siwek, Jakub Jończyk, Justyna Godyń, Barbara Malawska, Katarzyna Kieć-Kononowicz
    Conference:
    Mutalig COST Action CA15135 WG Meeting 2018 (year: 2018, pages: 63), Publisher: Local Organizing Committee
    Date:
    conference 15-16 March
    Status:
    Published

  2. THE INFLUENCE OF AN AMINE MOIETY FOR HISTAMINE H3 RECEPTOR AFFINITY AND MONOAMINE OXIDASE B INHIBITORY ACTIVITY

    Authors:
    Dorota Łażewska, Agata Siwek, Agnieszka Olejarz-Maciej, Agata Doroz-Płonka, Katarzyna Kieć-Kononowicz
    Conference:
    11th Joint Meeting on Medicinal Chemistry (year: 2019, pages: 90), Publisher: Faculty of Pharmacy in Hradec Kralowe
    Date:
    conference 43643
    Status:
    Published

  3. SEARCH FOR CHOLINESTERASE AND MAO B INHIBITORS AMONG TERT-AMYLPHENOXYALKYL DERIVATIVES - HISTAMINE H3 RECEPTOR LIGANDS

    Authors:
    Dorota Łażewska, Paula Zaręba, Agnieszka Olejarz-Maciej, Marek Bajda, Agata Doroz-Płonka, Agata Siwek, Kamil Kuder, Barbara Malawska, Katarzyna Kieć-Kononowicz
    Conference:
    European Histamine Research Society 47th Annual Meeting (year: 2018, pages: 68), Publisher: Local Organizing Committee
    Date:
    conference 31 May – 2 June
    Status:
    Published

  4. E-153 – THE NOVEL BIFUNCTIONAL H3 RECEPTOR ANTAGONIST/CHOLINESTERASE INHIBITOR REDUCES MEMORY IMPAIRMENT INDUCED BY SCOPOLAMINE AND MK-801

    Authors:
    Szcepan Mogilski, Karolina Pytka, Dorota Łażewska, Artur Świerczek, Barbara Filipek, Katarzyna Kieć-Kononowicz
    Conference:
    48th EHRS Annual Meeting (year: 2019, pages: 81), Publisher: Polskie Towarzystwo Chemii Medycznej
    Date:
    conference 43600
    Status:
    Published

  5. HUMAN HISTAMINE H3 RECEPTOR AFFINITY AND CHOLINE ESTERASE INHIBITORY ACTIVITIES OF (HOMO)PIPERIDINYL-HEXYLOXYBENZOPHENONE DERIVATIVES

    Authors:
    Dorota Łażewska, Paula Zaręba, Stefanie Hagenow, Maria Kaleta, Barbara Malawska, Holger Stark, Katarzyna Kieć-Kononowicz
    Conference:
    MuTaLig COST Action CA15135 3rd WG Meeting 2019 (year: 2019, pages: 40), Publisher: MuTaLig COST ACTION CA15135
    Date:
    conference 43519
    Status:
    Published

  6. AZEPANYLHEXYLOXY DERIVATIVES - HISTAMINE H3 RECEPTOR AFFINITY, CHOLINESTERASES INHIBITORY ACTIVITY AND ADME/TOX PREDICTION

    Authors:
    Dorota Łażewska, Paula Zaręba, Stefanie Hagenow, Maria Kaleta, Małgorzata Więcek, David Reiner, Annika Frank, Barbara Malawska, Holger Stark, Katarzyna Kieć-Kononowicz
    Conference:
    EFMC ACS MEDI Medicianl Chemistry Frontiers 2019 (year: 2019, pages: 144), Publisher: EFMC
    Date:
    conference 43626
    Status:
    Published

  7. HISTAMINE H3 RECEPTOR ANTAGONIST E177 ATTENUATES PENTYLENETETRAZOlE-INDUCED KINDLING PROGRESS AND ASSOCIATED MEMORY IMPAIRMENT AND OXIDATIVE STRESS IN RATS.

    Authors:
    Ala Alachkar, Sheikh Azimullah, Shreesh K. Ojha, Dorota Łażewska, Katarzyna Kieć-Kononowicz, Bassem Sadek
    Conference:
    48th EHRS Annual Meeting (year: 2019, pages: 42), Publisher: Polskie Towarzystwo Chemii Medycznej
    Date:
    conference 43600
    Status:
    Published

  8. HISTAMINE H3 RECEPTOR LIGANDS WITH MONOAMINE OXIDASES INHIBITORY ACTIVITY

    Authors:
    Kamil J. Kuder, Dorota Łażewska, Agnieszka Olejarz-Maciej, Maria Kaleta, Marek Bajda, Agata Siwek, Tadeusz Karcz, Agata Doroz-Płonka, Urszula Cichoń, Katarzyna Kieć-Kononowicz
    Conference:
    XVIIth Conference of the Polish Histamine Research Society (year: 2018, pages: 28), Publisher: Polskie Towarzystwo Badań nad Histaminą
    Date:
    conference 25-27 October
    Status:
    Published

  9. RECEPTORY H3 HISTAMINOWE - ATRAKCYJNY CEL POSZUKIWAŃ SUBSTANCJI BIOLOGICZNIE AKTYWNYCH

    Authors:
    Dorota Łażewska, Maria Kaleta, Stephan Schwed, Szczepan Mogilski, Agnieszka Olejarz-Maciej, Alaa Alachkar, Agata Siwek, Tadeusz Karcz, Kamil Kuder, Agata Doroz-Płonka, Bassem Sadek, Holger Stark, Katarzyna Kieć-Kononowicz
    Conference:
    IV sympozjum Szkoła Chemii Medycznej (year: 2019, pages: W7), Publisher: Uniwersytet Medyczny we Wrocławiu
    Date:
    conference 43733
    Status:
    Published

  10. PIPERIDINE (AZEPANE)-ALKOXY-BIPHENYLCARBONITRILES AS HISTAMINE H3 RECEPTOR LIGANDS

    Authors:
    Katarzyna Kieć-Kononowicz, Holger Stark, Dorota Łażewska, Maria Kaleta, Gniewomir Latacz, Ewelina Honkisz, Kamil Kuder, Agnieszka Olejarz, Annamaria Lubelska
    Conference:
    European Histamine Research Society 47th Annual Meeting (year: 2018, pages: 69), Publisher: Local Organizing Committee
    Date:
    conference 31 May – 2 June
    Status:
    Published

  11. CHOLINESTERASES INHIBITION OF NOVEL HISTAMINE H3 RECEPTOR LIGANDS AS MULTIFUNCTIONAL LIGANDS ON ALZHEIMER'S DISEASE

    Authors:
    Paula Zaręba, Marek Bajda, Dorota Łażewska, David Reiner, Annika Frank, Holger Stark, Katarzyna Kieć-Kononowicz, Barbara Malawska
    Conference:
    IX Konwersatorium Chemii Medycznej (year: 2018, pages: P136), Publisher: Local Organizing Committee
    Date:
    conference 13-15 września
    Status:
    Published

  12. BIPHENYL DERIVATIVES – HISTAMINE H3 RECEPTOR LIGANDS AND CHOLINESTERASE INHIBITORS

    Authors:
    Dorota Łażewska, Paula Zaręba, Szczepan Mogilski, Małgorzata Więcek, Barbara Filipek, Barbara Malawska, Katarzyna Kieć-Kononowicz
    Conference:
    A Satellite Symposium of WCP2018 2nd Joint Symposium of European and Japanese Histamine Research Societies (year: 2018, pages: 58), Publisher: Local Organizing Committee
    Date:
    conference 7-9 July
    Status:
    Published

  13. MONOAMINE OXIDASE B INHIBITION OF NOVEL ANALOGS AND DERIVATIVES OF 1-[3-(4-TERT-BUTYL-PHENOXY)PROPYL]PIPERIDINE

    Authors:
    Agnieszka Olejarz, Urszula Cichoń, Dorota Łażewska, Tadeusz Karcz, Agata Siwek, Holger Stark, Katarzyna Kieć-Kononowicz
    Conference:
    XVIIth Conference of the Polish Histamine Research Society (year: 2018, pages: 30), Publisher: Polskie Towarzystwo Badań nad Histaminą
    Date:
    conference 25-27 October
    Status:
    Published

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Graphic design and implementation: Jakub Piotrowski