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

2016/23/B/NZ7/02327

Keywords:

histamine H3 receptor Alzheimer disease acetylcholinesterase butyrylcholinesterase monoamino oxidase B

Descriptors:

  • NZ7_4: Prevention in population health
  • NZ7_14: Pharmacy, pharmacotherapy, pharmacology
  • ST5_16:

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):

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 (Y-m-d): 2017-07-25

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

Information in the final report

  • Publication in academic press/journals (9)
  • Articles in post-conference publications (13)
  1. 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 (rok: 2018, tom: 28, strony: 175-196), Wydawca: Taylor&Trancis Group
    Status:
    Published
    DOI:
    10.1080/13543776.2018.1424135 - link to the publication
  2. 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 (rok: 2020, tom: 185, strony: 111785), Wydawca: Science Direct
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2019.111785 - link to the publication
  3. 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 (rok: 2018, tom: 19, strony: 3386), Wydawca: MDPI
    Status:
    Published
    DOI:
    10.3390/ijms19113386 - link to the publication
  4. 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 (rok: 2021, tom: 26, strony: 3580), Wydawca: MDPI
    Status:
    Published
    DOI:
    10.3390/molecules26123580 - link to the publication
  5. 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 (rok: 2020, tom: 21, strony: 3411), Wydawca: MDPI
    Status:
    Published
    DOI:
    10.3390/ijms21103411 - 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 (rok: 2020, tom: 30, strony: 127147), Wydawca: Science Direct
    Status:
    Published
    DOI:
    10.1016/j.bmcl.2020.127147 - link to the publication
  7. 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 (rok: 2020, tom: 207, strony: 112743), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2020.112743 - link to the publication
  8. 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 (rok: 2018, tom: 28, strony: 3596-3600), Wydawca: Elsevier
    Status:
    Published
  9. 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 (rok: 2021, tom: 114, strony: 105129), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.bioorg.2021.105129 - link to the publication
  1. 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 (rok: 2018, ), Wydawca: Polskie Towarzystwo Badań nad Histaminą
    Data:
    konferencja 25-27 October
    Status:
    Published
  2. 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 (rok: 2018, ), Wydawca: Local Organizing Committee
    Data:
    konferencja 15-16 March
    Status:
    Published
  3. 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 (rok: 2018, ), Wydawca: Local Organizing Committee
    Data:
    konferencja 7-9 July
    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 (rok: 2019, ), Wydawca: Polskie Towarzystwo Chemii Medycznej
    Data:
    konferencja 43600
    Status:
    Published
  5. 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 (rok: 2018, ), Wydawca: Local Organizing Committee
    Data:
    konferencja 31 May – 2 June
    Status:
    Published
  6. 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 (rok: 2019, ), Wydawca: Faculty of Pharmacy in Hradec Kralowe
    Data:
    konferencja 43643
    Status:
    Published
  7. 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 (rok: 2019, ), Wydawca: EFMC
    Data:
    konferencja 43626
    Status:
    Published
  8. 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 (rok: 2018, ), Wydawca: Local Organizing Committee
    Data:
    konferencja 13-15 września
    Status:
    Published
  9. 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 (rok: 2019, ), Wydawca: Polskie Towarzystwo Chemii Medycznej
    Data:
    konferencja 43600
    Status:
    Published
  10. 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 (rok: 2018, ), Wydawca: Polskie Towarzystwo Badań nad Histaminą
    Data:
    konferencja 25-27 October
    Status:
    Published
  11. 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 (rok: 2019, ), Wydawca: MuTaLig COST ACTION CA15135
    Data:
    konferencja 43519
    Status:
    Published
  12. 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 (rok: 2018, ), Wydawca: Local Organizing Committee
    Data:
    konferencja 31 May – 2 June
    Status:
    Published
  13. 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" (rok: 2019, ), Wydawca: Uniwersytet Medyczny we Wrocławiu
    Data:
    konferencja 43733
    Status:
    Published