Unusual 5-HT6 receptor ligands

2014/13/B/NZ7/02210

Keywords

Descriptors

  • NZ7_14: Farmacja, farmakoterapia, farmakologia
  • ST5_23: Chemia organiczna
  • NZ2_7: Bioinformatyka

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

Instytut Farmakologii PAN

Voivodeship: małopolskie

Other projects carried out by the institution »

Principal investigator (from the host institution)

prof. Andrzej Jacek Bojarski

Number of co-investigators in the project: 8

Call

OPUS 7 – announced on 2014-03-17

Amount awarded
604 680 PLN
Project start date
2015-02-04
Project end date
2017-08-03
Project duration
30 months (the same as in the proposal)
Project status
Project settled

Equipment purchased [PL]

  1. Detektor UV dla chromatografii RD4: 250-280-RI-Cond z akcesoriami lub o porównywalnych parametrach. Cost: 30 000 PLN
  2. Komputer do obsługi detektora UV. Cost: 3 000 PLN
  3. Mieszadło magnetyczne Heidolph MR Hei-Tec. Cost: 12 000 PLN
  4. Wyparka rotacyjna, Hei-VAP Value. Cost: 17 000 PLN
  5. Zestaw bloków grzejnych do ogrzewania mieszanin reakcyjnych firmy Radleys. Cost: 8 000 PLN
  6. Zestaw kolumn do stacji chromatograficznej VersaFlash, (VersaPak C18, VersaPak Silica). Cost: 10 000 PLN

Information in the final report

Publication in academic press/journals (3)

  1. Low-basicity 5-HT7 Receptor Agonists Synthesized Using the van Leusen Multicomponent Protocol

    Authors:
    Hogendorf,A.S.; Hogendorf,A.; Kurczab,R.; Satala,G.; Lenda,T.; Walczak,M.; Latacz,G.; Handzlik,J.; Kiec-Kononowicz,K.; Wieronska,J.M.; Wozniak,M.; Cieslik,P.; Bugno,R.; Staron,J.; Bojarski,A.J.
    Academic press:
    Scientific Reports (year: 2017, volume: 7, pages: 1444), Publisher: Nature Publishing Group
    Status:
    Published
    DOI:
    10.1038/s41598-017-00822-4 – link to the publication
  2. The effect of the intramolecular C-H center dot center dot center dot O interactions on the conformational preferences of bis-arylsulfones-5-HT6 receptor antagonists and beyond

    Authors:
    Kalinowska-Tłuścik J., Staroń J., Krawczuk A., Mordalski S., Warszycki D., Satała G., Hogendorf A. S., Bojarski A. J.
    Academic press:
    RSC Advances (year: 2018, volume: 8, pages: 18672-18681), Publisher: Royal Society of Chemistry
    Status:
    Published
    DOI:
    10.1039/c8ra03107j – link to the publication
  3. A pyrano[2,3,4-cd]indole as a scaffold for selective non-basic 5-HT6R ligands

    Authors:
    Staroń,J.; Mordalski,S.; Warszycki,D.; Satała,G.; Hogendorf,A.; Bojarski,A.J.
    Academic press:
    ACS Medicinal Chemistry Letters (year: 2017, volume: 8, pages: 390-394), Publisher: American Chemical Society
    Status:
    Published
    DOI:
    10.1021/acsmedchemlett.6b00482 – link to the publication

Articles in post-conference publications (7)

  1. New non-basic 5-HT6 Receptor Ligands

    Authors:
    Bugno, R.; Staroń, J.; Hogendorf, A.; Satała, G.; Warszycki, D.; Mordalski, S.; Bojarski, A.J.
    Conference:
    VII Conversatory on Medicinal Chemistry (year: 2015, pages: PP7), Publisher: Uniwersytet Medyczny w Lublinie
    Date:
    conference 17-19.09.2015
    Status:
    Published
    DOI:
    link to the publication
  2. Synthesis and evaluation of a new indole-based series as nonbasic 5-HT6 receptor ligands

    Authors:
    Bugno,R.; Staroń,J.; Hogendorf,A.S.; Satała,G.; Warszycki,D.; Mordalski,S.; Bojarski,A.J.
    Conference:
    VIIIth Conversatory on Medicinal Chemistry (year: 2016, pages: P95), Publisher: Uniwersytet Medyczny w Lublinie
    Date:
    conference 15-17.09.2016
    Status:
    Published
    DOI:
    link to the publication
  3. An analysis of molecular interactions between the 5-HT6 receptor and non-basic ligands

    Authors:
    Warszycki, D.; Rataj, K.; Bojarski, A.J.
    Conference:
    VII Conversatory on Medicinal Chemistry (year: 2015, pages: P102), Publisher: Uniwersytet Medyczny w Lublinie
    Date:
    conference 17-19.09.2015
    Status:
    Published
    DOI:
    link to the publication
  4. A non-basic 5-HT6R antagonists

    Authors:
    Staroń,J.; Satała,G.; Warszycki,D.; Bojarski,A.J.
    Conference:
    XXIV EFMC International Symposium on Medicinal Chemistry (year: 2016, pages: 244, P306), Publisher: EFMC
    Date:
    conference 28.08-01.09.2016
    Status:
    Published
  5. Design, synthesis and structure-activity relationships of 1-(arylsulfonyl)-1H-indole derivatives as non-basic 5-HT6 receptor ligands

    Authors:
    Bugno,R.; Staroń,J.; Hogendorf,A.S.; Satała,G.; Warszycki,D.; Mordalski,S.; Bojarski,A.J.
    Conference:
    XXIV EFMC International Symposium on Medicinal Chemistry (year: 2016, pages: 245), Publisher: EFMC
    Date:
    conference 28.08-01.09.2016
    Status:
    Published
  6. Molecular mechanism of activity of non-basic ligands of 5-HT6 receptors

    Authors:
    Mordalski, S.; Warszycki, D.; Staron, J.; Hogendorf, A.; Bugno, R.; Satała, G.; Bojarski, A.J.
    Conference:
    2nd Central European Biomedical Congress (CEBC) (year: 2016, pages: 40), Publisher: Instytut Farmakologii PAN
    Date:
    conference 15-18.06.2016
    Status:
    Published
  7. Non-basic antagonists of the 5-HT6 receptor - a structure-activity relationship study

    Authors:
    Kalinowska-Tłuścik,J.; Staroń,J.; Bojarski,A.J.
    Conference:
    VIIIth Conversatory on Medicinal Chemistry (year: 2016, pages: PP17), Publisher: Uniwersytet Medyczny w Lublinie
    Date:
    conference 15-17.09.2016
    Status:
    Published
    DOI:
    link to the publication

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Graphic design and implementation: Jakub Piotrowski