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    In vitro anti-Helicobacter pylori, anti-urease and anti-gastric cancer activities of novel hydrazones
    (Elsevier B.V., 2024) Maryam, Zahra; Kaya, Betül; Bostancı, Hayrani Eren; Kısa, Dursun; Çelik, İsmail; Acar Çevik, Ulviye; Kaplancıklı, Zafer Asım
    In this study, new hydrazone derivatives were synthesized by taking into account the virulence factor of the urease in the urease-positive microorganism H. pylori. The structure of synthesized compounds 3a-3j was confirmed using 1H NMR, 13C NMR and elemental analyses. After structure confirmations all compounds were evaluated for in vitro urease inhibitory and anti-H. pylori activities. Furthermore, since H. pylori infection is associated with gastric cancer, the effects of the synthesized compounds against two different gastric cancer cell lines (SNU1 and AGS) were also evaluated. Amongst the series, two compounds 3c and 3j were found to be excellent inhibitors of urease, having IC50 values of 9.813 ± 0.403 µM and 11.407 ± 0.393 µM, better than the standard thiourea (IC50 = 13.428 ± 0.587 µM), whereas the remaining compounds displayed moderate activity. Compounds 3c and 3d were found to be the most active in the series against H. pylori with MIC values 4 µg/mL and 5 µg/mL. Next, compounds were evaluated as anti-gastric cancer activity and the compounds 3c and 3j were more potent than reference drug cisplatin against SNU1 and AGS. The docking study was executed to analyzed the interaction between the active site of the urease and the compounds 3c and 3j. When the all activities (anti-H. pylori, anti-urease and anti-gastric cancer activities) examined, it was found that the presence of the nitro group, which is an electron withdrawing group, in the 5th position of the thiophene ring (compound 3c) increased all activities. From the structure-activity relationship, it has been observed that the compound 3c showed excellent potential for anti-H. pylori, anti-gastric cancer and can be alternative therapy in the future. © 2024
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    Synthesis, and docking studies of novel tetrazole-S-alkyl derivatives as antimicrobial agents
    (Taylor and Francis Ltd., 2023) Acar Çevik, Ulviye; Celik, Ismail; Işık, Ayşen; Gül, Ülküye Dudu; Bayazıt, Gizem; Bostancı, Hayrani Eren; Özkay, Yusuf
    A series of novel tetrazole-S-alkyl-piperazine derivatives were synthesized and evaluated for their antifungal activity against C. albicans (ATCC 24433), C. krusei (ATCC 6258) and C. parapsilosis (ATCC 22019) and antibacterial activity against E. coli (ATCC 25922), S. marcescens (ATCC 8100), K. pneumoniae (ATCC 13883), P. aeruginosa (ATCC 27853), E. faecalis (ATCC 2942), B. subtilis (ATCC), S. aureus (ATCC 29213), S. epidermidis (ATCC 12228). Among the synthesized compounds, 1-(4-cycylohexylpiperazin-1-yl)-2-((1-methyl-1H-tetrazol-5-yl)thio)ethan-1-one (2b) (MIC = 7.81 µg/mL) and 1-(4-(4-chlorobenzyl)piperazin-1-yl)-2-((1-methyl-1H-tetrazol-5-yl)thio)ethan-1-one (2f) (MIC = 3.90 µg/mL) displayed significant antifungal activity and compared to reference drugs voriconazole and fluconazole. Besides, compound 2b has showed also higher antibacterial activity against E. faecalis (ATCC 2942) as a reference drug azithromycin, with a MIC value of 3.90 µg/mL, and compound 2d was found to be effective against S. epidermidis (ATCC 12228) as the same reference drug, with a MIC value of 7.81 µg/mL. All the derivatives were efficiently synthesized by a two-step process. The structure of the newly synthesized compounds was elucidated by their 1H NMR, 13C NMR, LC-MS/MS, and elemental analysis. In this study, the detailed synthesis, spectroscopic and biological evaluation data are reported. Molecular docking studies of all compounds were performed with the sterol 14-alpha demethylase enzyme of C. albicans, the target enzyme of azole antifungal drugs. © 2022 Taylor & Francis Group, LLC.