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    Wyświetlanie 1-3 z 3
    Tytuł:
    Synthesis and anticancer activity evaluation of some new derivatives of 2-(4-benzoyl-1-piperazinyl)-quinoline and 2-(4-cinnamoyl-1-piperazinyl)-quinoline.
    Autorzy:
    Kubica, Krzysztof P.
    Taciak, Przemyslaw P.
    Czajkowska, Agnieszka
    Sztokfisz-Ignasiak, Alicja
    Wyrebiak, Rafal
    Podsadni, Piotr
    Mlynarczuk-Bialy, Izabela
    Malejczyk, Jacek
    Mazurek, Aleksander P.
    Powiązania:
    https://bibliotekanauki.pl/articles/895388.pdf
    Data publikacji:
    2018-08-31
    Wydawca:
    Polskie Towarzystwo Farmaceutyczne
    Tematy:
    anticancer activity
    cytotoxicity assay
    2-quinoline
    cell migration assay
    Opis:
    In this study we designed and synthesized twenty new derivatives of 2-(4-benzoyl-1-piperazinyl)-quinoline and 2-(4-cinnamoyl-1-piperazinyl)-quinoline with potential anticancer activity. The structures of synthesized compounds were confirmed by 1H and 13C NMR spectroscopy and MS spectrometry. The activity of novel compounds was evaluated in the cell viability assay as well as in the wound healing assay. Presented data show that examined substances have anticancer activity in cell culture. Seven compounds which showed a high rate of cell growth inhibition were selected for further studies. Three of them strongly reduced growth of B16F10 cells. The novel compounds constitute a good base for further studies and optimization of structure for new therapeutically effective anti-cancerous drugs.
    Źródło:
    Acta Poloniae Pharmaceutica - Drug Research; 2018, 75, 4; 891-901
    0001-6837
    2353-5288
    Pojawia się w:
    Acta Poloniae Pharmaceutica - Drug Research
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Synthesis, Characterization and Biological evaluation of 6-substituted-2-(substituted-phenyl)-quinoline derivatives bearing 4-amino-1,2,4-triazole-3-thiol ring at C-4 position
    Autorzy:
    Vaghasiya, R. G.
    Ghodasara, H. B.
    Vachharajani, P. R.
    Shah, V. H.
    Powiązania:
    https://bibliotekanauki.pl/articles/412211.pdf
    Data publikacji:
    2014
    Wydawca:
    Przedsiębiorstwo Wydawnictw Naukowych Darwin / Scientific Publishing House DARWIN
    Tematy:
    Quinoline, 4-amino-1,2,4-triazole-3-thiol
    therapeutic agents
    antimicrobial assai
    Opis:
    Quinoline derivatives represent one of the most active classes of compounds possesses wide spectrum biodynamic activities and use as potent therapeutic agents. In this research work, a synthesis, characterization and biological evaluation of 6-substituted-2-(substituted-phenyl)-quinoline derivatives bearing 4-amino-1,2,4-triazole-3-thiol ring at C-4 position is described. The synthesis of quinoline derivatives is carried out by the reaction of substituted quinoline-4-carbohydrazides with a mixture of carbon disulphide and potassium hydroxide which further react with hydrazine hydrate to give final compounds. All of these compounds were screened for their in vitro antimicrobial assay against gram (+ve), gram (-ve) bacteria and fungi activity compared with standard drugs viz., Ampicilin, Chloramphenicol, Ciprofloxacin, Norfloxacin, Griseofulvin and Nystatin at different concentrations.
    Źródło:
    International Letters of Chemistry, Physics and Astronomy; 2014, 8; 30-37
    2299-3843
    Pojawia się w:
    International Letters of Chemistry, Physics and Astronomy
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Właściwości wewnątrzcząsteczkowych wiązań wodorowych w wybranych N-tlenkach pochodnych chinoliny
    Intramolecular hydrogen bonds properties in selected N-oxides of quinoline derivatives
    Autorzy:
    Jezierska, Aneta
    Panek, Jarosław J.
    Błaziak, Kacper
    Powiązania:
    https://bibliotekanauki.pl/articles/171511.pdf
    Data publikacji:
    2019
    Wydawca:
    Polskie Towarzystwo Chemiczne
    Tematy:
    DFT
    teoria funkcjonału gęstości
    MP2
    metoda rachunku zaburzeń drugiego rzędu Møllera-Plesseta
    CPMD
    dynamika molekularna Cara-Parrinello
    wewnątrzcząsteczkowe wiązanie wodorowe
    N-tlenki pochodnych chinoliny
    density functional theory
    Møller-Plesset second order perturbation method
    Car-Parrinello molecular dynamics
    intramolecular HB
    N-oxides of quinoline derivatives
    Opis:
    In the current article we would like to summarize our research shedding light onto properties of intramolecular hydrogen bonds present in N-oxide quinoline derivatives. The compounds for the current study were chosen to contain diverse types of hydrogen bonds. Therefore, in the current study we analyze three kinds of hydrogen bonding and their properties. It is well known, that the presence of intramolecular hydrogen bonds stabilizes conformations of molecules. Substituent effects (inductive and steric) influence the strength of the H-bonding as well as its features. Moreover, the intramolecular hydrogen bond in the studied N-oxides belongs to the family of resonance assisted hydrogen bonds (RAHB). Our short overview presents the summary of results obtained for twelve N-oxides of quinoline derivatives. Quantum-chemical simulations were performed on the basis of static models (classical DFT and MP2 approaches) as well as ab initio molecular dynamics (Car-Parrinello MD). The metadynamics method was applied to reproduce the maps of free energy for the motion of the bridged proton. The computations were performed in the gas and in the crystalline phases. Electronic ground state is a natural framework in which chemical compounds exist most of the time. However, in many chemical species we observe a spontaneous internal reorganization of their chemical bonds and atoms e.g. proton transfer phenomenon and the appearance of tautomeric forms already in the ground state. Therefore, it was interesting to investigate some N-oxides in the excited electron state knowing that they exhibit excited- state-induced proton transfer (ESIPT effect). At the end of the article we draw some conclusions related to the intramolecular H-bond properties present in the discussed N-oxides of quinoline derivatives.
    Źródło:
    Wiadomości Chemiczne; 2019, 73, 1-2; 75-95
    0043-5104
    2300-0295
    Pojawia się w:
    Wiadomości Chemiczne
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
      Wyświetlanie 1-3 z 3

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