Yazar "Tas, Omer" seçeneğine göre listele

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    Öğe
    Biological, computational evaluation of novel benzofuranyl derivatives as acetylcholinesterase and butyrylcholinesterase
    (Taylor & Francis Ltd, 2024) Usanmaz, Hande; Tas, Omer; Ekinci, Deniz; Uba, Abdullahi Ibrahim; Atmaca, Ufuk
    Aim: A highly efficient one-step method has been developed for the synthesis of benzofuranyl derivatives from 2-benzoylcyclohexane-1-carboxylic acid derivatives using chlorosulfonyl isocyanate. This novel method provides a practical, cost-effective and efficient approach. Materials & methods: The inhibitory effects of benzofuranyl derivatives on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes were investigated. Ki values were determined to range from 0.009 to 0.61 mu M for AChE and 0.28 to 1.60 mu M for BChE. Molecular docking analysis provided insights into the interaction modes and binding patterns of these compounds with AChE and BChE. Conclusion: Kinetic findings of our study suggest that some of our compounds exhibited more effective low micromolar inhibition compared with the reference, and these derivatives could be to design more powerful agents.
  • [ X ]
    Öğe
    Inhibitory effects of sulfenimides on human and bovine carbonic anhydrase enzymes
    (Taylor & Francis Ltd, 2023) Yakan, Hasan; Bilir, Gurkan; Cakmak, Sukriye; Tas, Omer; Karakullukcu, Nalan Turkoz; Soydan, Ercan; Kutuk, Halil
    A series of sulfenimide derivatives (1a-i) were investigated as inhibitors of human (hCA-I, hCA-II) and bovine (bCA) carbonic anhydrase enzymes. The compounds were synthesised by the reaction of substituted thiophenols with phthalimide by means of an effective, simple and eco-friendly method and the structures were confirmed by IR, H-1 NMR, C-13 NMR, MS and elemental analysis. All derivatives except for the methyl derivative (1b) exhibited effective inhibitory action at low micromolar concentrations on human isoforms, but only four derivatives (1e, 1f, 1h, 1i) inhibited the bovine enzyme. The bromo derivative (1f) was found to be strongest inhibitor of all three enzymes with KI values of 0.023, 0.044 and 20.57 mu M for hCA-I, hCA-II and bCA, respectively. Results of our study will make valuable contributions to carbonic anhydrase inhibition studies for further investigations since inhibitors of this enzyme are important molecules for medicinal chemistry.