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    Öğe
    Synthesis and biological evaluation of quinoline-triazole and quinolone-triazole conjugates
    (Tubitak Scientific & Technological Research Council Turkey, 2018) Gumus, Aysegul; Okumus, Veysi
    One-pot synthesis of novel quinoline- and quinolone-substituted 1,2,3-triazoles has been performed from the key intermediates, quinoline- and quinolone-substituted propargyl derivatives 1-3 (48%-88% yields). The antioxidant properties of the newly synthesized compounds, 1a-1c, 2a-2c, and 3a-3c, were evaluated by monitoring DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging abilities, metal chelating effects, and reducing power. The scavenging effects of compounds on the free radical decreased in the order of 3b > 3a > 1b and were found to be 36.3%, 34.9%, and 27.6% at the concentration of 500 mu g/mL, respectively. All of the compounds showed low chelating capacity. Furthermore, the antibacterial activity was studied against gram-positive and gram-negative bacteria and the DNA binding ability of the compounds was evaluated with calf thymus DNA using agarose gel electrophoresis.
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    Öğe
    Synthesis of 2-substituted 8-propargyloxyquinoline derivatives and determination of their antioxidant, antibacterial, and DNA binding activities
    (Tubitak Scientific & Technological Research Council Turkey, 2018) Gumus, Aysegul; Okumus, Veysi; Gumus, Selcuk
    2-Substituted 8-propargyloxyquinoline derivatives have been synthesized from 2-substituted-8-hydroxyquinolines by O-propargylation method (30%-98% yields). The newly synthesized compounds were tested for in vitro antioxidant activities such as DPPH radical scavenging, ferrous chelating, and reducing power activities. The maximum radical scavenging (46.5%) and reducing power activities were obtained from 1 and maximum ferrous chelating effect was obtained from 6 (72.1%) at the concentration of 500 mu g/mL. To indicate DNA binding activity of the complexes calf thymus DNA was used. The compounds were also evaluated for their antimicrobial activity against three gram-positive and three gram-negative bacteria. Compounds 3 and 5 exhibited antibacterial activity against all tested gram-positive bacteria.
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    Öğe
    Synthesis, biological evaluation of antioxidant-antibacterial activities and computational studies of novel anthracene- and pyrene-based Schiff base derivatives
    (Tubitak Scientific & Technological Research Council Turkey, 2020) Gumus, Aysegul; Okumus, Veysi; Gumus, Selcuk
    Schiff base derivatives with anthracene- and pyrene-based units, Al-A6 and P1-P6 were synthesized (89%-99% yields). Schiff base derivatives were designed to possess an heterocyclic moiety on one side to enhance the coordination ability towards metals. To investigate the biological assay of the newly synthesized compounds, their DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging, metal chelating, reducing power, antibacterial and DNA binding activities were tested. A6 (63.1%) showed the maximum free radical scavenging activity among all. However, compound P3 at concentration of 200 mu g/mL possessed the highest metal chelating (45.8%) activity and power of reduction. In addition, P3 and A6 showed antibacterial activity against all bacteria tested and both compounds were very well bound to CT-DNA. Density functional theory method with B3LYP/6-311++ G(d,p) basis set was performed to get information about the structural and electronic properties of the present compounds. In addition, the metal coordination properties of the dimers of the parent Schiff bases were investigated through interactions with Zn2+.