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    Cytotoxic effects, carbonic anhydrase isoenzymes, ?-glycosidase and acetylcholinesterase inhibitory properties, and molecular docking studies of heteroatom-containing sulfonyl hydrazone derivatives
    (Taylor & Francis Inc, 2021) Celebioglu, Hasan Ufuk; Erden, Yavuz; Hamurcu, Fatma; Taslimi, Parham; Senturk, Ozan Sanli; Ozmen, Ummuhan Ozdemir; Tuzun, Burak
    Today, interest in studies on the search for new drugs to be used in diseases such as cancer, cardiovascular diseases, neurodegenerative diseases and diabetes, as well as prevention of microbial inflammation is increasing day by day. Emerging biological and pharmacological effects of sulfonyl hydrazone derivative compounds reveal their importance. In the present study, heteroatom-containing sulfonyl hydrazone derivatives have been studied for their anticancer and antimicrobial properties, as well as their effects on enzymes that could play roles in Alzheimer's dissease and diabetes. High doses of the tested compounds significantly decreased the cell viabilities of breast cancer (MCF-7) and prostate cancer (PC-3) cell lines. Furthermore, all compounds possessed antimicrobial activities against very common bacteriaE. coliandS. aureus. These compounds were good inhibitors of the alpha-glycosidase, human carbonic anhydrase I and II isoforms and acetylcholinesterase enzyme withK(i)values in the range of 1.14 +/- 0.14-3.63 +/- 0.26 nM for alpha-glycosidase, 66.05 +/- 9.21-125.45 +/- 11.54 nM for hCA I, 89.14 +/- 10.43-170.22 +/- 26.05 nM for hCA II and 754.03 +/- 73.22-943.92 +/- 58.15 nM for AChE, respectively. Molecular docking method was used to theoretically compare biological activities of sulfonyl hydrazone derivatives against enzymes. The theoretical results were compared with the experimental results. Thus, these compounds have strong biological activities. Communicated by Ramaswamy H. Sarma
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    Eco-friendly and potential colin esterase enzyme inhibitor agent sulfonyl hydrazone series: Synthesis, Bioactivity Screening, DFT, ADME properties, and Molecular Docking study
    (Journal of Molecular Structure, 4 April 2023) Ozmen, Ummuhan Ozdemir; Tuzun, Burak; Ayan, Esra Bilen; Cevrimli, Bekir Sıtkı
    In this study, new compounds containing the sulfonamide group and having inhibitory activity on cholinesterase enzymes (AChE, BChE) were synthesized. For this purpose, three new sulfonylhydrazone compounds were synthesized from different alkylsulfonic acid hydrazide and N’-(4-diethylamino) salicylaldehyde and designed by the green chemistry method in shorter time and more environmentally friendly. The structures of the synthesized compounds were characterized by elemental analysis (CHNS), 1HNMR , 13CNMR , and FT-IR. The effects of the synthesized sulfonylhydrazone derivatives (4Dea-salesh, 4Dea-salpsh, 4Dea-salbsh) on acetylcholinesterase and butyrylcholinesterase enzymes were investigated. According to the results, all synthesized compounds showed inhibitory effect on AChE and BChE enzymes. In particular, 4Dea-salbsh exhibited the best activity with an IC50 value of 9.549±0.75 μM on AChE. The Molecules were optimized by B3LYP, HF, and M062X methods with 6–31++g(d,p) basis sets. Then, their activities against biological materials namely acetylcholinesterase (AChE) (PDB ID: 4M0E and 1OCE) and butyrylcholinesterase (BChE) (PDB ID: 5NN0 and 6R6V), were compared. Molecular docking studies were performed to evaluate the binding interactions between the compounds and the enzymes. Subsequently, ADME/T properties were investigated to test the drug properties.