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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Design and synthesis of new rifampicin analogs as a source of effective bacterial RNA polymerase inhibitors

2011/03/B/ST5/01014

Keywords:

ansamycin antibiotics rifampicin rifampicin modifications antibacterial activity structure-activity relationship 1D and 2D NMR mass spectrometry FT-IR molecular modelling

Descriptors:

  • ST5_16:
  • ST5_23:
  • ST5_20:

Panel:

ST5 - Materials: materials synthesis, structure-properties relations, advanced and functional materials with designed properties, (macro)molecular architecture, material engineering

Host institution :

Uniwersytet im. Adama Mickiewicza, Wydział Chemii

woj. wielkopolskie

Other projects carried out by the institution 

Principal investigator (from the host institution):

dr hab. Piotr Przybylski 

Number of co-investigators in the project: 3

Call: OPUS 2 - announced on 2011-09-15

Amount awarded: 615 000 PLN

Project start date (Y-m-d): 2012-09-04

Project end date (Y-m-d): 2015-09-03

Project duration:: 36 months (the same as in the proposal)

Project status: Project settled

Equipment purchased [PL]

  1. "Przenośny zestaw do modelowania molekularnego z oprogramowaniem" (laptop + programy do modelowania molekularnego Scigress Explorer+ADF) (24 000 PLN)
  2. Waga analityczna Ohause PA 214C/1 (14 000 PLN)
  3. Program do edycji i obróbki widm NMR MestreNova (3 500 PLN)
  4. Zestaw do HPLC wraz z detektorami UV-vis i detektorem koronowym i kolumnami chromatograficznymi (350 000 PLN)
  5. kuweta do FT-IR (10 000 PLN)
  6. Notebook Dell Latitude (5 000 PLN)
  7. Wyparka rotacyjna, Hei-Vap Advantage z systemem próżniowym SC920 (2 mBar) (20 000 PLN)

Information in the final report

  • Publication in academic press/journals (6)
  • Articles in post-conference publications (5)
  1. Regioselective Long-Range Proton Transfer in New Rifamycin Antibiotics: A Process in which Crown Ethers Act as Stronger Brønsted Bases than Amines
    Authors:
    K. Pyta, P. Przybylski, F. Bartl
    Academic press:
    ChemPhysChem (rok: 2015, tom: 16, strony: 938 –942), Wydawca: John Wiley & Sons, Inc.
    Status:
    Published
    DOI:
    10.1002/cphc.201402892 - link to the publication
  2. The effect of complexation of 3-formylrifamycin SV macrocyclic ether derivatives with metal cations and small nitrogen-containing organic molecules on antibacterial activity against S. aureus and S. epidermidis
    Authors:
    Piotr Przybylski, Krystian Pyta, Dominika Czerwonka, Marcelina M. Kubicka, Marzena Gajecka
    Academic press:
    Bioorganic & Medicinal Chemistry Letters (rok: 2015, tom: 25, strony: 3903-3909), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.bmcl.2015.07.043 - link to the publication
  3. Structure–activity relationship studies of new rifamycins containing L-amino acid esters as inhibitors of bacterial RNA polymerases
    Authors:
    D. Czerwonka, J. Domagalska, K. Pyta, M. M. Kubicka, P. Pecyna, M. Gajecka, P. Przybylski
    Academic press:
    European Journal of Medicinal Chemistry (rok: 2016, tom: w druku, strony: w druku), Wydawca: Elsevier
    Status:
    Accepted for publication
    DOI:
    10.1016/j.ejmech.2016.03.061 - link to the publication
  4. 13C and 15N CP/MAS, 1H–15N SCT CP/MAS and FTIR spectroscopy as tools for qualitative detection of the presence of zwitterionic and non-ionic forms of ansa-macrolide 3-formylrifamycin and its derivatives in solid state
    Authors:
    Piotr Przybylski, Krystian Pyta, Katarzyna Klich, Wojciech Schilf, Bohdan Kamieński
    Academic press:
    Magnetic Resonance in Chemistry (rok: 2014, tom: 52, strony: 10–21), Wydawca: John Wiley & Sons, Ltd.
    Status:
    Published
    DOI:
    10.1002/mrc.4028 - link to the publication
  5. A new model of binding of rifampicin and its amino analogues as zwitterions
    Authors:
    Krystian Pyta, Piotr Przybylski, Katarzyna Klich and Joanna Stefańska
    Academic press:
    Organic&Biomolecular Chemistry (rok: 2012, tom: 10, strony: 8283–8297), Wydawca: Royal Society of Chemistry
    Status:
    Published
    DOI:
    10.1039/c2ob26317c - link to the publication
  6. Structure and evaluation of antibacterial and antitubercular properties of new basic and heterocyclic 3-formylrifamycin SV derivatives obtained via 'click chemistry' approach
    Authors:
    Krystian Pyta, Katarzyna Klich, Joanna Domagalska and Piotr Przybylski
    Academic press:
    European Journal of Medicinal Chemistry (rok: 2014, tom: 84, strony: 651-676), Wydawca: Elsevier
    Status:
    Published
    DOI:
    10.1016/j.ejmech.2014.07.066 - link to the publication
  1. From the proton transfer within Rifamycin antibiotics to mechanism of inhibition of bacterial RNA polymerase dependent on DNA
    Authors:
    Piotr Przybylski, Krystian Pyta, Katarzyna Klich, Joanna Domagalska, Maria Gdaniec, Barbara Wicher
    Conference:
    BIT's 4th Annual International Conference of Medichem-2013 (ICM-2013) with Nobel Laureates' Forum (rok: 2013, ), Wydawca: Organizing Committee of ICM-2013
    Data:
    konferencja 13.11-16.11
    Status:
    Published
  2. Regioselective proton transfer within 3-formylrifamycin SV derivatives
    Authors:
    P. Przybylski, K. Pyta, J. Domagalska, K. Klich
    Conference:
    Ogólnopolskie sympozjum Chiralność - od cząstki elementarnej do Uniwersum" (rok: 2013, ), Wydawca: Wydział Chemii UAM, PTCH
    Data:
    konferencja 07.06.
    Status:
    Published
  3. Investigation of proton transfer process in rifampicin in the solid state
    Authors:
    K. Pyta, P. Przybylski, K. Klich, W. Schilf, B. Kamienski
    Conference:
    BIT's 4th Annual International Conference of Medichem-2013 (ICM-2013) with Nobel Laureates' Forum (rok: 2013, ), Wydawca: Organizing Comittee of ICM-2013
    Data:
    konferencja 13.11.-16.11
    Status:
    Published
  4. Investigation of proton transfer process in rifampicin in the solid state
    Authors:
    Krystian Pyta, Piotr Przybylski, Katarzyna Klich, Wojciech Schilf, Bohdan Kamieński
    Conference:
    Central European School on Physical Organic Chemistry- "From Molecule to material chemistry for the future" (rok: 2013, ), Wydawca: Faculty of Chemistry, University of Wroclaw, PTCH
    Data:
    konferencja 27.05-31.05
    Status:
    Published
  5. Structure and antibacterial activity of new amino derivatives of 3-formylrifamicin SV containing crown ethers and L- aminoacids
    Authors:
    Dominika Czerwonka, Joanna Domagalska, Marcelina Kubicka, Marzena Gajęcka, Krystian Pyta, Piotr Przybylski
    Conference:
    58 Zjazd Polskiego Towarzystwa Chemicznego w Gdańsku (rok: 2015, ), Wydawca: Uniwersytet Gdański
    Data:
    konferencja 21-25.09
    Status:
    Published

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