Basic Information
ID: ALA4765317
Journal: Eur J Med Chem
Title: Novel bacterial topoisomerase inhibitors derived from isomannide.
Authors: Okumu A,Lu Y,Dellos-Nolan S,Papa JL,Koci B,Cockroft NT,Gallucci J,Wozniak DJ,Yalowich JC,Mitton-Fry MJ
Abstract: A series of Novel Bacterial Topoisomerase Inhibitors (NBTIs) employing a linker derived from isomannide were synthesized and evaluated. Reduced hERG inhibition was observed compared to structure-matched analogues with different linkers, and compound 6 showed minimal proarrhythmic potential using an in vitro panel of cardiac ion channels. Compound 6 also displayed excellent activity against fluoroquinolone-resistant MRSA (MIC = 2 μg/mL) and other Gram-positive pathogens.
CiteXplore: 32402932
DOI: 10.1016/j.ejmech.2020.112324
Patent ID: ┄
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