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 vanilloid type 1 receptor (TRPV1) antagonists in the search for substances with wide-spectrum of anticonvulsant and antinociceptive activity in the preclinical studies

2017/27/B/NZ7/00249

Keywords:

TRPV1 antagonists amide derivatives anticonvulsant activity antinociceptive activity

Descriptors:

  • NZ7_14: Pharmacy, pharmacotherapy, pharmacology

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. Krzysztof Kamiński 

Number of co-investigators in the project: 17

Call: OPUS 14 - announced on 2017-09-15

Amount awarded: 1 528 266 PLN

Project start date (Y-m-d): 2018-07-31

Project end date (Y-m-d): 2023-07-30

Project duration:: 60 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. CHŁODZIARKO-ZAMRAŻARKA (11 094 PLN)
  2. System do wysokosprawnej chromatografii cieczowej (HPLC) (234 000 PLN)
  3. Termostat cyrkulacyjny.
  4. WAGA ANALITYCZNA (3 929 PLN)
  5. Komputer przenośny (6 000 PLN)
  6. MIESZADŁA MAGNETYCZNE (3 sztuki) (12 361 PLN)
  7. NOTATNIK ELEKTORNICZNY (3 679 PLN)
  8. Komputer przenośny.

Information in the final report

  • Publication in academic press/journals (4)
  • Articles in post-conference publications (10)
  1. Discovery of (R)-N-benzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide [(R)-AS-1], a novel orally bioavailable EAAT2 modulator with drug-like properties and potent antiseizure activity in vivo
    Authors:
    Abram, M.; Jakubiec, M.; Reeb, K.; Cheng, M. H.; Gedschold, R.; Rapacz, A.; Mogilski, S.; Socała, K.; Nieoczym, D.; Szafarz, M.; Latacz, G.; Szulczyk, B.; Kalinowska-Tłuścik, J.; Gawel, K.; Esguerra, C. V.; Wyska, E.; Müller, C. E.; Bahar, I.; Fontana, A. C. K.; Wlaź, P.; Kamiński, R. M.; Kamiński, K.
    Academic press:
    Journal of Medicinal Chemistry (rok: 2022, tom: 65, strony: 11703–11725.), Wydawca: ACS
    Status:
    Published
    DOI:
    10.1021/acs.jmedchem.2c00534 - link to the publication
  2. In vivo and in vitro characterization of close analogs of compound KA-11, a new antiseizure drug candidate
    Authors:
    Andres-Mach, M.; Zagaja, M.; Szala-Rycaj, J.; Szewczyk, A.; Abram, M.; Jakubiec, M.; Ciepiela, K.; Socała, K.; Wlaź, P.; Latacz 4, G.; Khan, N.; Kamiński, K.
    Academic press:
    Interational Journal of Molecular Sciences (rok: 2023, tom: 24, strony: 8302), Wydawca: MDPI
    Status:
    Published
    DOI:
    10.3390/ijms24098302 - link to the publication
  3. TRPV1 channel as a potential molecular target for development of new antiseizure drugs - what do we know today?
    Authors:
    Socała K., Jakubiec M., Abram M., Mlost J., Starowicz K., Kamiński, R.M., Ciepiela K., Andres-Mach M., Zagaja M., Metcalf C.S., Zawadzki P., Wlaź P., Kamiński K.
    Academic press:
    Pharmacological Reviews (rok: 2023, tom: -, strony: -), Wydawca: ASPET
    Status:
    Submitted
  4. Phenylglycinamide Derivatives with Hybrid Structure as Candidates for New Broad-Spectrum Anticonvulsants
    Authors:
    Jakubiec M., Abram M., Zagaja M., Andres-Mach M., Szewczyk A., Latacz G., Szulczyk B., Socała K., Nieoczym D., Wlaź P., Metcalf C.S., Wilcox K., Kamiński R.M., Kamiński K.
    Academic press:
    Cells (rok: 2022, tom: 11, strony: 1862), Wydawca: MDPI
    Status:
    Published
    DOI:
    10.3390/cells11121862 - link to the publication
  1. New phenyl-glycinamide derivatives with hybrid structure as candidates on new effective anticonvulsants
    Authors:
    Marcin Jakubiec, Michał Abram, Mirosław Zagaja, Marta Andres-Mach, Aleksandra Szewczyk, Gniewomir Latacz, Bartłomiej Szulczyk, Katarzyna Socała, Dorota Nieoczym, Piotr Wlaź, Krzysztof Kamiński
    Conference:
    X Konwersatorium Chemii Medycznej (rok: 2021, ), Wydawca: Uniwersytet Medyczny w Lublinie
    Data:
    konferencja 3-5.09.2021
    Status:
    Published
  2. Discovery of compound (R)-AS-1, the first in class broad-spectrum antiseizure drug candidate with innovative mechanism of action and superb safety profile
    Authors:
    Kamiński K., Abram M., Jakubiec M., Mogilski S., Latacz G., Andres-Mach M., Zagaja M., Kamiński R.M.
    Conference:
    16th EILAT Conference on New Antiepileptic Drugs and Devices (rok: 2022, ), Wydawca: The Hebrew University of Jerusalem
    Data:
    konferencja 22-25.05
    Status:
    Published
  3. New TRPV1 Antagonists as Candidates for Effective Anticonvulsant and Antinociceptive Agents
    Authors:
    Krzysztof Kamiński, Marcin Jakubiec, Mirosław Zagaja, Marta Andres-Mach, Szczepan Mogilski, Gniewomir Latacz
    Conference:
    2nd Molecules Medicinal Chemistry Symposium (MMCS): Facing Novel Challenges in Drug Discovery (rok: 2019, ), Wydawca: Licensee MDPI, Basel, Switzerland
    Data:
    konferencja 43600
    Status:
    Published
  4. DEVELOPMENT OF NEW ANTISEIZURE AND ANTINOCICEPTIVE AGENTS IN A GROUP OF MODIFIED ALANINAMIDE DERIVATIVES
    Authors:
    Marcin Jakubiec, Michał Abram, Mirosław Zagaja, Marta Andres-Mach, Aleksandra Szewczyk, Szczepan Mogilski, Ewelina Honkisz-Orzechowska, Gniewomir Latacz, Katarzyna Socała, Dorota Nieoczym, Piotr Wlaź, Krzysztof Kamiński
    Conference:
    RICT 2023, 57th International Conference on Medicinal Chemistry, Lille, France (rok: 2023, ), Wydawca: SCT
    Data:
    konferencja 05-07.07
    Status:
    Published
  5. New TRPV1 channel antagonist with anticonvulsant and antinociceptive activity
    Authors:
    Marcin Jakubiec, Mirosałw Zagaja, Marta Andres-Mach, Aleksandra Szewczyk, Michał Abram, Szczepan Mogliski, Gniewomir Latacz, Bartłomiej Szulczyk, Krzysztof Kamiński
    Conference:
    11th Joint Meeting on Medicinal Chemistry 2019 (rok: 2019, ), Wydawca: GUARANT International spol. s r.o.
    Data:
    konferencja 43643
    Status:
    Published
  6. New phenyl-glycinamide derivatives with hybrid structure as new effective anticonvulsant candidates
    Authors:
    Marcin Jakubiec, Michał Abram, Mirosław Zagaja, Marta Andres-Mach, Aleksandra Szewczyk, Gniewomir Latacz, Bartłomiej Szulczyk, Katarzyna Socała, Dorota Nieoczym, Piotr Wlaź, Krzysztof Kamiński
    Conference:
    7th International Electronic Conference on Medicinal Chemistry (rok: 2021, ), Wydawca: MDPI
    Data:
    konferencja 1-30.11.2021
    Status:
    Published
  7. TRPV1 channel as a novel molecular target for new anticonvulsants
    Authors:
    Marcin Jakubiec, Michała Abram, Szczepan Mogilski, Bartłomiej Szulczyk, Krzysztof Kamiński
    Conference:
    XI Multidyscyplinarna Konferencja Nauki o Leku (rok: 2018, ), Wydawca: Instytut Farmaceutyczny, ul. Rydygiera 8, 071-9793 Warszawa
    Data:
    konferencja 43418
    Status:
    Published
  8. NEW PHENYLGLYCINAMIDE DERIVATIVES AS CANDIDATES FOR EFFECTIVE ANTISEIZURE DRUGS WITH POTENT ANTINOCICEPTIVE PROPERTIES
    Authors:
    Krzysztof Kamiński, Marcin Jakubiec, Michał Abram, Marta Andres-Mach, Mirosław Zagaja, Szczepan Mogilski, Gniewomir Latacz, Rafał M. Kamiński
    Conference:
    RICT 2023, 57th International Conference on Medicinal Chemistry, Lille, France (rok: 2023, ), Wydawca: SCT
    Data:
    konferencja 05-07.07
    Status:
    Published
  9. NOVEL INTEGRATED PYRROLIDINE-2-ONE HYBRID COMPOUNDS WITH BROAD-SPECTRUM ANTISEIZURE ACTIVITY IN THE PRECLINICAL STUDIES
    Authors:
    ał Abram, Marcin Jakubiec, Mirosław Zagaja, Marta Andres-Mach, Aleksandra Szewczyk, Katarzyna Socała, Piotr Wlaź, Kamiński Kamiński
    Conference:
    RICT 2023, 57th International Conference on Medicinal Chemistry, Lille, France (rok: 2023, ), Wydawca: SCT
    Data:
    konferencja 05-07.07
    Status:
    Published
  10. New phenyl-glycinamide derivatives with hybrid structure as candidates for new broad-spectrum anticonvulsants with additional antinociceptive properties
    Authors:
    Jakubiec M., Abram M., Zagaja M., Andres-Mach M., Szewczyk A., Mogilski S., Latacz G., Szulczyk B., Socała K., Nieoczym D., Wlaź P., Kamiński K
    Conference:
    16th EILAT Conference on New Antiepileptic Drugs and Devices (rok: 2022, ), Wydawca: The Hebrew University of Jerusalem
    Data:
    konferencja 22-25.05
    Status:
    Published