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Novel bacterial topoisomerase inhibitors derived from isomannide.
Okumu, Antony; Lu, Yanran; Dellos-Nolan, Sheri; Papa, Jonathan L; Koci, Bryan; Cockroft, Nicholas T; Gallucci, Judith; Wozniak, Daniel J; Yalowich, Jack C; Mitton-Fry, Mark J.
Afiliação
  • Okumu A; Division of Medicinal Chemistry and Pharmacognosy. The Ohio State University, Columbus, OH, 43210, USA.
  • Lu Y; 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.
  • Papa JL; Division of Pharmaceutics and Pharmacology. The Ohio State University, Columbus, OH, 43210, USA.
  • Koci B; Eurofins Panlabs. St. Charles, MO, 63304, USA.
  • Cockroft NT; Division of Medicinal Chemistry and Pharmacognosy. The Ohio State University, Columbus, OH, 43210, USA.
  • Gallucci J; Department of Chemistry and Biochemistry. 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.
  • Yalowich JC; Division of Pharmaceutics and Pharmacology. 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.
Eur J Med Chem ; 199: 112324, 2020 Aug 01.
Article em En | MEDLINE | ID: mdl-32402932
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 (MIC90 = 2 µg/mL) and other Gram-positive pathogens.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Compostos Bicíclicos Heterocíclicos com Pontes / Inibidores da Topoisomerase / Bactérias Gram-Positivas / Antibacterianos Idioma: En Revista: Eur J Med Chem Ano de publicação: 2020 Tipo de documento: Article País de afiliação: Estados Unidos
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Compostos Bicíclicos Heterocíclicos com Pontes / Inibidores da Topoisomerase / Bactérias Gram-Positivas / Antibacterianos Idioma: En Revista: Eur J Med Chem Ano de publicação: 2020 Tipo de documento: Article País de afiliação: Estados Unidos