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    Quinoline-imidazo[1,2-a]pyridine conjugates as potential antioxidant agents: Synthesis, experimental and theoretical approaches
    (Elsevier, 2026) Bouria, Houria; Alliouche, Hayette; Mermer, Arif; Sirin, Yakup; Tuzun, Burak; Bensegueni, Rafik; Chouiter, Mohamed Imed
    N-heterocyclic compounds such as quinolines and imidazopyridines are very important structures in medicinal chemistry, especially for drug development. In this work, a series of novel quinoline-imidazo[1,2-a]pyridines hybrids (IMP1-10) were synthesized from 3-(quinolin-3-yl) oxirane-2,2-carbonitriles (1-10) via a nucleophilic ring-opening reaction and were characterized by conventional analytical techniques. The antioxidant capacity of the synthesized compounds was investigated using the DPPH, FRAP and ABTS methods, and it was found that IMP-7 exhibited the best DPPH and FRAP activity with an IC50 values of 0,33 +/- 0,05 & micro;M and 2387,45 +/- 23,25 mu mol TE/g, respectively. In the course of the analysis of the ABTS assay results, IMP-10 was found to demonstrate the highest activity, with an IC50 value of 0.67 +/- 0.04 & micro;M. The antioxidant mechanism properties of the most potent compounds IMP-7, IMP-8 and IMP-10 were calculated with the Gaussian package program using HF/6-31++G(d,p) basis set.
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    Synthesis of 1,3-Disubtitituted Tetrahydropyrimidinium Salts and Determination of Their Biological Properties and Molecular Docking
    (Wiley-V C H Verlag Gmbh, 2024) Karaca, Emine Ozge; Gurbuz, Nevin; Demir, Yeliz; Tuzun, Burak; Ozdemir, Ismail; Gulcin, Ilhami
    Several of 3,4,5,6-tetrahydropyrimidinium salts with 1-methyl functionalization are produced. By using techniques for 1H-NMR, 13C-NMR, and IR spectroscopy, all compounds were investigated. Additionally, these compounds' abilities to block enzymes were looked into. They had a highly effective inhibitory effect on the isoenzymes of carbonic anhydrases I and II, butyrylcholinesterase (BChE), and acetylcholinesterase (AChE). Ki values were found in the range of 57.43 +/- 7.09-170.09 +/- 50.91 nM for AChE, 7.19 +/- 0.42-69.08 +/- 2.44 nM for BChE, and 46.48 +/- 5.74-203.38 +/- 46.15 nM for hCA I, and 30.19 +/- 4.03-171.96 +/- 30.27 nM for hCA II. As a result, 1,3-disubtitituted tetrahydroprimidinium salts exhibited potent inhibition profiles toward indicated metabolic enzymes. One of the most important methods for designing and creating novel, potent medications to treat Alzheimer's disease (AD) worldwide is the synthesis and discovery of new AChE and BChE inhibitors. The activities of synthesized 3,4,5,6-tetrahydropyrimidinium salts were compared against various proteins that are crystal structure of AChE (PDB ID: 4 M0E), crystal structure of BChE (PDB ID: 5NN0), crystal structure of hCA I (PDB ID: 2CAB), and crystal structure of hCA II (PDB ID: 3DC3), and then the drug properties of these molecules were examined. In this study, we have designed and synthesized a series of 1,3-disubtitituted tetrahydropyrimidinium salts were synthesized and characterized by IR and NMR spectra. These compounds were evaluated against the AChE, BChE, hCA I and hCA II enzymes. These compounds showed good enzyme inhibition profiles. The activities of the investigated 1,3-disubstituted tetrahydropyrimidinium salts were compared to the theoretical calculations results using molecular docking. image