Novel bacterial topoisomerase inhibitors derived from isomannide


European Journal of Medicinal Chemistry


Antony Okumu, Yanran Lu, Sheri Dellos-Nolan, Jonathan L. Papa, Bryan Koci, Nicholas T. Cockroft, Judith Gallucci, Daniel J. Wozniak, Jack C. Yalowich, Mark J. Mitton-Fry



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 (MIC90 = 2 μg/mL) and other Gram-positive pathogens.

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