New N -phenyl-4,5-dibromopyrrolamides as DNA gyrase B inhibitors
Nace Zidar, Helena Macut, Tihomir Tomašič, Lucíja Peterlin Mašič, Janez Ilaš, Anamarija Zega, Päivi Tammela, D. Kikelj
Abstract
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Nace Zidar, Helena Macut, Tihomir Tomašič, Lucíja Peterlin Mašič, Janez Ilaš, Anamarija Zega, Päivi Tammela, D. Kikelj
Abstract
Open-access reader
topoisomerase IV were in the low micromolar range. However, the compounds evaluated did not show significant antibacterial activities against selected Gram-positive and Gram-negative bacteria. Our results indicate that for potent inhibition of DNA gyrase, a combination of polar groups on the carboxylic end of the molecule and substituents that reach into the 'lipophilic floor' of the enzyme is required.
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topoisomerase IV were in the low micromolar range. However, the compounds evaluated did not show significant antibacterial activities against selected Gram-positive and Gram-negative bacteria. Our results indicate that for potent inhibition of DNA gyrase, a combination of polar groups on the carboxylic end of the molecule and substituents that reach into the 'lipophilic floor' of the enzyme is required.
Key concepts: DNA gyrase, Novobiocin, Topoisomerase IV, Topoisomerase, DNA, Escherichia coli, Antibiotics, Chemistry