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Synthesis, Antimicrobial Activities of New Sulfonamidobenzoxazoles and Molecular Docking Studies on Escherichia coli TEM-1 ?-Lactamase
(Croatian Chemical Soc, 2017) Ertan-Bolelli, Tugba; Bolelli, Kayhan; Okten, Suzan; Kaynak-Onurdag, Fatma; Aki-Yalcin, Esin; Yalcin, Ismail
beta-Lactam antibiotics are frequently used for treatment of multi-drug resistant microbial infections and the most common mechanism of resistance against these antibiotics is bacterial beta-lactamase production. Herein, we reported the design, synthesis and in vitro antimicrobial activities of some new 2-substituted-5-(2,4-dinitrophenylsulfonamido) benzoxazole derivatives. Compounds TN1, TN2, and TN3 were found to be significantly active against E. coli isolate which contains extended spectrum beta-lactamase enzyme at the MIC value of 8 mu g mL(-1) and that is 4-fold higher than the reference drug ampicillin. We performed molecular docking studies into active site of Escherichia coli TEM-1 beta-lactamase enzyme in order to predict the protein-ligand interactions. According to the docking results, compounds TN1, TN2, and TN3 showed strong interactions between the important active site residues which are responsible for the catalytic mechanism of TEM-1 beta-lactamase enzyme and a good correlation is found with the experimental data.