Quinine bis-conjugates with quinolone antibiotics and peptides: synthesis and antimalarial bioassay

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Abstract

Benzotriazole-mediated syntheses led to novel bis-conjugates of quinine with quinolone antibiotics and amino acid linkers which were successfully prepared by two alternative routes with excellent yields and retention of chirality. These bis conjugates retain in vitro antimalarial activity with IC(50) values ranging from 12 to 207 nM, similar to quinine itself.

Original languageEnglish (US)
Pages (from-to)8985-93
Number of pages9
JournalOrganic and Biomolecular Chemistry
Volume10
Issue number45
DOIs
StatePublished - Dec 7 2012

Keywords

  • Anti-Bacterial Agents
  • Antimalarials
  • Chemistry Techniques, Synthetic
  • Inhibitory Concentration 50
  • Peptide Fragments
  • Plasmodium falciparum
  • Quinine
  • Quinolones
  • Triazoles
  • Journal Article
  • Research Support, Non-U.S. Gov't

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