WoS İndeksli Yayınlar Koleksiyonu
Permanent URI for this collectionhttps://hdl.handle.net/20.500.14627/6
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Article Comprehensive Proteomic and Metabolomic Analysis of Novel Substituted Fluoroquinolone Derivatives in Escherichia Coli Isolates(John Wiley and Sons Ltd, 2026) Nigiz Ş.; Kulabaş N.; Türe A.; Kablan S.; Koçak E.; Özkul C.; Küçükgüzel İ.; Koçak, Engin; Nigiz, Şeyma; Kablan, Sevilay Erdoğan; Özkul, Ceren; Kulabaş, Necla; Küçükgüzel, İlkay; Türe, AslıAntimicrobial resistance is one of the most important global problems, and new antibiotic requirements have been emerging as a key point in this issue. In the present work, we focused on the efficiency of two novel promising fluoroquinolone derivatives on resistant Escherichia coli isolates at the molecular level. Their mode of action and adaptation process were evaluated by using proteomics and metabolomics analysis. Proteomics analysis showed that two compounds have an effect mainly on the ribosomal process and energy metabolism. Moreover, we observed compounds that affect various important antimicrobial targets, such as ribosomal subunits, phosphotransacetylase, and chaperone proteins. In metabolomics analysis, we found that compounds altered bacterial metabolism directly. Pathway analysis showed that cofactor biosynthesis and energy metabolism were affected mainly by undertreated groups. Our experiments demonstrated that novel fluoroquinolone derivatives have promising results at the molecular level and results will contribute to further studies. © 2026 John Wiley & Sons Ltd.Article Synthesis, Molecular Modeling, Anti-Cancer and COX-1/2 Inhibitory Activities of Novel Thiazolidinones Containing Benzothiazole Core(Bangladesh Pharmacological Society, 2024) Kulabas, Necla; Guven, Cansu Tamniku; Duracık, Merve; Bingol Ozakpinar, Ozlem; Küçükgüzel, İlkay; Ozakpinar, Ozlem BingolIn this study, new 1,3-thiazolidin-4-one derivatives containing arylmethylene groups in the 5-position were obtained from 6-(trifluoromethoxy)-1,3-benzo-thiazol-2-amine (riluzole). Synthesized compounds were characterized by spectral data and elemental analysis. In vitro, cytotoxic activities of the synthesized molecules were evaluated against the human lung cancer (A549) and human prostate cancer (PC-3) cell lines. Compounds were also tested on mouse embryonic fibroblast cells (NIH/3T3) to determine selectivity. Ten target compounds 3-12 were also screened for their COX-1 and COX-2 inhibitory activities. Of these compounds, 4 showed the highest COX-2 inhibition at 10 μM. Molecular docking calculations were performed to understand the binding interactions of compounds with COX-1 and COX-2 proteins. In silico studies of the tested compounds represented important binding modes that may be responsible for their anti-cancer activity via selective inhibition of the COX-2 enzyme. ADMET predictions were conducted to assess the drug-like properties of the novel compounds. © 2024 Elsevier B.V., All rights reserved.