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Synthesis and anti-staphylococcal activity of novel bacterial topoisomerase inhibitors with a 5-amino-1,3-dioxane linker moiety.
Li, Linsen; Okumu, Antony; Dellos-Nolan, Sheri; Li, Zoe; Karmahapatra, Soumendrakrishna; English, Anthony; Yalowich, Jack C; Wozniak, Daniel J; Mitton-Fry, Mark J.
Affiliation
  • Li L; Division of Medicinal Chemistry and Pharmacognosy, The Ohio State University, Columbus, OH 43210, USA.
  • Okumu A; Division of Medicinal Chemistry and Pharmacognosy, The Ohio State University, Columbus, OH 43210, USA.
  • Dellos-Nolan S; Microbial Infection and Immunity, The Ohio State University, Columbus, OH 43210, USA.
  • Li Z; Division of Pharmacology, The Ohio State University, Columbus, OH 43210, USA.
  • Karmahapatra S; Division of Pharmacology, The Ohio State University, Columbus, OH 43210, USA.
  • English A; Division of Pharmacology, The Ohio State University, Columbus, OH 43210, USA.
  • Yalowich JC; Division of Pharmacology, The Ohio State University, Columbus, OH 43210, USA.
  • Wozniak DJ; Microbial Infection and Immunity, The Ohio State University, Columbus, OH 43210, USA; Department of Microbiology, The Ohio State University, Columbus, OH 43210, USA.
  • Mitton-Fry MJ; Division of Medicinal Chemistry and Pharmacognosy, The Ohio State University, Columbus, OH 43210, USA. Electronic address: mitton-fry.1@osu.edu.
Bioorg Med Chem Lett ; 28(14): 2477-2480, 2018 08 01.
Article in En | MEDLINE | ID: mdl-29871847
ABSTRACT
Novel bacterial type II topoisomerase inhibitors (NBTIs) constitute a promising new class of antibacterial agents. We report a series of NBTIs with potent anti-staphylococcal activity and diminished hERG inhibition. Dioxane-linked compound 9 demonstrated MICs ≤1 µg/mL against both methicillin-susceptible (MSSA) and -resistant Staphylococcus aureus (MRSA), accompanied by reduced hERG inhibition as compared to cyclohexane- or piperidine-linked analogs.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Quinolines / DNA Topoisomerases, Type II / Potassium Channel Blockers / Dioxanes / Methicillin-Resistant Staphylococcus aureus / Topoisomerase II Inhibitors / Anti-Bacterial Agents Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2018 Document type: Article Affiliation country: Estados Unidos
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Quinolines / DNA Topoisomerases, Type II / Potassium Channel Blockers / Dioxanes / Methicillin-Resistant Staphylococcus aureus / Topoisomerase II Inhibitors / Anti-Bacterial Agents Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2018 Document type: Article Affiliation country: Estados Unidos