Sürdürülebilir Kalkınma Amaçları

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• MakaleAçık Erişim2026/r/gumushane/13715
  Synthesis, Characterization, Biological Properties, and Sensor Applications of Novel Thiosemicarbazone Derivatives

  Gezegen, Hayreddin; Özbek, Oguz; Topal, Meryem; Şahin, Hatice; Koçyiğit, Ümit M.

  In this study, novel thiosemicarbazone derivative molecules (5a–j) were synthesized. The characterization of the synthesized molecules was carried out using 1H–, 13C–NMR, FT–IR, and Q–TOF spectroscopic techniques. Then, the inhibitory effect of these compounds was examined for human carbonic anhydrase I and II (hCA I, and II) and acetylcholinesterase (AChE). The hCA I II, and AChE were efficiently inhibited by synthesized thiosemicarbazone derivatives, with Ki values in the range of 0.293–1.666 µM for hCA I, 0.298–1.332 µM for hCA II, and 52.51–138.63 µM for AChE, respectively. Finally, the sensor properties of the synthesized thiosemicarbazone derivatives were investigated. The newly synthesized thiosemicarbazone derivative molecules exhibited high selectivity towards Pb2+ ions. The sensor prepared with 5a from these molecules had a Nernstian behavior of 28.8 ± 1.5 mV/decade and a low detection limit of 2.86 × 10−6 M in a wide concentration range of 1.0 × 10−1–1.0 × 10−5 M. The newly proposed sensor also had a wide pH working range (5.0–10.0), a very fast response time (5 s), and good reproducibility. The newly fabricated sensors were used as indicator electrodes for the potentiometric titration of Pb2+ ions with ethylenediaminetetraacetic acid (EDTA) and were successfully applied for the determination of Pb2+ ion content in different water samples.

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• MakaleAçık Erişim2025/r/gumushane/12209
  Novel Sulfonylhydrazones With Sulfonate Ester Framework: Promising Dual Inhibitors of AChE and hCAs

  Öztürk, Cansu; Balci, Neslihan; Aslan, Osman Nuri; Kalay, Erbay

  Alzheimer's disease (AD) is a progressive neurodegenerative disorder that affects millions of individuals worldwide. Treatment strategies for AD vary depending on cognitive and behavioral symptoms, with cholinergic replacement therapy using acetylcholinesterase (AChE) inhibitors being one of the primary approaches. Recent studies have also identified human carbonic anhydrases (hCAs) as significant therapeutic targets for AD, offering new opportunities for the development of innovative treatments. Carbonic anhydrase inhibitors have been shown to prevent early mitochondrial damage and inhibit H2O2 production, thereby reducing amyloid plaque formation. Building on the promising potential of hydrazones particularly sulfonyl hydrazones as anticholinesterase agents, we synthesized 12 novel chlorine-substituted sulfonyl hydrazone compounds containing aryl sulfonate ester groups. These compounds were evaluated for their inhibitory effects on AChE, hCA I, and hCA II enzymes. The synthesized compounds exhibited low nanomolar inhibitory activity, with Ki values ranging from 9.58 ± 2.22 to 104.04 ± 23.82 nM for AChE, 9.12 ± 2.21 to 477.63 ± 218.52 nM for hCA I, and 17.54 ± 7.74 to 564.62 ± 213.98 nM for hCA II. Notably, compound 6 showed strong inhibitory activity against hCA I (Ki = 9.12 ± 2.21 nM; acetazolamide (AZA) = 26.54 ± 3.11 nM) and hCA II (Ki = 17.54 ± 7.74 nM; AZA = 21.73 ± 2.42 nM), whereas compound 4 exhibited superior AChE inhibition (Ki = 9.58 ± 2.22 nM; TAC = 23.12 ± 2.05 nM). The chemical structures of the synthesized compounds were characterized using advanced spectroscopic techniques, including FT-IR, 1H-NMR, and 13C-NMR spectroscopy.

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• MakaleYalnız künye2024/r/gumushane/11970
  Sulfonamide derivatives with benzothiazole scaffold: Synthesis and carbonic anhydrase I–II inhibition properties

  Öztürk, Cansu; Kalay, Erbay; Gerni, Serpil; Balci, Neslihan; Tokali, Feyzi Sinan; Aslan, Osman Nuri; Polat, Emrah

  The secondary sulfonamide derivatives containing benzothiazole scaffold (1–10) were synthesized to determine their inhibition properties on two physiologically essential human carbonic anhydrases isoforms (hCAs, EC, 4.2.1.1), hCA I, and hCA II. The inhibitory effects of the compounds on hCA I and hCA II isoenzymes were investigated by comparing their IC50 and Ki values. The Ki values of compounds (1–10) against hCA I and hCA II are in the range of 0.052 ± 0.022–0.971 ± 0.280 and 0.025 ± 0.010–0.682 ± 0.335, respectively. Some of these inhibited the enzyme more effectively than the standard drug, acetazolamide. In particular, compounds 5 and 4 were found to be most effective on hCA I and hCA II.

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