@article {537, title = {Design and synthesis of novel 1H-tetrazol-5-amine based potent antimicrobial agents: DNA topoisomerase IV and gyrase affinity evaluation supported by molecular docking studies}, journal = {European Journal of Medicinal Chemistry}, volume = {156}, year = {2018}, pages = {631 - 640}, abstract = {A total of 14 of 1,5-disubstituted tetrazole derivatives were prepared by reacting appropriate thiourea and sodium azide in the presence of mercury (II) chloride and triethylamine. All compounds were evaluated in\ vitro for their antimicrobial activity. Derivatives 10 and 11 showed the highest inhibition against Gram-positive and Gram-negative strains (standard and hospital strains). The observed minimal inhibitory concentrations values were in the range of 1{\textendash}208 μM (0.25{\textendash}64 μg/ml). Inhibitory activity of 1,5-tetrazole derivatives 10 and 11 against gyrase and topoisomerase IV isolated from S.\ aureus was studied. Evaluation was supported by molecular docking studies for all synthesized derivatives and reference ciprofloxacin. Moreover, selected tetrazoles (2, 3, 5, 6, 8, 9, 10 and 11) were evaluated for their cytotoxicity. All tested compounds are non-cytotoxic against HaCaT and A549 cells (CC50 <= 60 μM).}, keywords = {1H-tetrazol-5-amine, Antimicrobial activity, Cytotoxicity, DNA gyrase, molecular docking, Topoisomerase type IV}, issn = {0223-5234}, doi = {https://doi.org/10.1016/j.ejmech.2018.07.041}, url = {http://www.sciencedirect.com/science/article/pii/S022352341830597X}, author = {Daniel Szulczyk and Micha{\l} A. Dobrowolski and Piotr Roszkowski and Anna Bielenica and Joanna Stefa{\'n}ska and Michal Kolinski and Sebastian Kmiecik and Micha{\l} J{\'o}{\'z}wiak and Ma{\l}gorzata Wrzosek and Wioletta Olejarz and Marta Struga} } @article {529, title = {Synthesis, structural and antimicrobial studies of type II topoisomerase-targeted copper(II) complexes of 1,3-disubstituted thiourea ligands}, journal = {Journal of Inorganic Biochemistry}, volume = {182}, year = {2018}, pages = {61 - 70}, abstract = {A series of Cu(II) complexes of 3-(trifluoromethyl)phenylthiourea derivatives was synthesized. Their structural properties were investigated by spectroscopic techniques (infrared and electron paramagnetic resonance), as well as molecular modeling. All studied coordination compounds are mononuclear complexes containing two chelating ligands bonded to the metal cation via S and deprotonated N atoms. The new chelates were evaluated for their antimicrobial potency. The complex of 1-(3,4-dichlorophenyl)-3-[3-(trifluoromethyl)phenyl]thiourea (3) presented the highest activity against Gram-positive pathogens, even stronger than the activity of its non-complexed counterpart and the reference drug. The compound also prevented the biofilm formation of methicillin-resistant and standard strains of staphylococcal cocci. The title derivatives were found to be effective inhibitors of DNA gyrase and topoisomerase IV isolated from Staphylococcus aureus. The binding modes of the ligand L3 with DNA gyrase and topoisomerase IV were presented.}, keywords = {Copper complexes, DNA gyrase, docking, FTIR, Thiourea}, issn = {0162-0134}, doi = {https://doi.org/10.1016/j.jinorgbio.2018.01.005}, url = {http://www.sciencedirect.com/science/article/pii/S016201341730692X}, author = {Anna Bielenica and Aleksandra Drzewiecka-Antonik and Pawe{\l} Rejmak and Joanna Stefa{\'n}ska and Micha{\l} Koli{\'n}ski and Sebastian Kmiecik and Bogdan Lesyng and Marta W{\l}odarczyk and Piotr Pietrzyk and Marta Struga} }