2019•MedChemCommOpen access

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

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Abstract

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.

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Available abstract

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

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New N -phenyl-4,5-dibromopyrrolamides as DNA gyrase B inhibitors — Research Paper | ScholarLens