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Title: Solid-phase synthesis and biological evaluation of piperazine-based novel bacterial topoisomerase inhibitors
Authors: Flagstad, Thomas
Pedersen, Mette T.
Jakobsen, Tim H.
Felding, Jakob
Tolker-Nielsen, Tim
Givskov, Michael
Qvortrup, Katrine
Nielsen, Thomas E.
Keywords: Science::Biological sciences
Issue Date: 2022
Source: Flagstad, T., Pedersen, M. T., Jakobsen, T. H., Felding, J., Tolker-Nielsen, T., Givskov, M., Qvortrup, K. & Nielsen, T. E. (2022). Solid-phase synthesis and biological evaluation of piperazine-based novel bacterial topoisomerase inhibitors. Bioorganic & Medicinal Chemistry Letters, 57, 128499-.
Journal: Bioorganic & Medicinal Chemistry Letters 
Abstract: There is an emerging global need for new and more effective antibiotics against multi-resistant bacteria. This situation has led to massive industrial investigations on novel bacterial topoisomerase inhibitors (NBTIs) that target the vital bacterial enzymes DNA gyrase and topoisomerase IV. However, several of the NBTI compound classes have been associated with inhibition of the hERG potassium channel, an undesired cause of cardiac arrhythmia, which challenges medicinal chemistry efforts through lengthy synthetic routes. We herein present a solid-phase strategy that rapidly facilitates the chemical synthesis of a promising new class of NBTIs. A proof-of-concept library was synthesized with the ability to modulate both hERG affinity and antibacterial activity through scaffold substitutions.
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2021.128499
Research Centres: Singapore Centre for Environmental Life Sciences and Engineering 
Rights: © 2021 The Authors. Published by Elsevier Ltd. This is an open access article under the CC BY license (
Fulltext Permission: open
Fulltext Availability: With Fulltext
Appears in Collections:SCELSE Journal Articles

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