Synthesis and antimalarial bioassay of quinine - peptide conjugates

Chem Biol Drug Des. 2013 Oct;82(4):361-6. doi: 10.1111/cbdd.12134.

Abstract

Amino acid and peptide conjugates of quinine were synthesized using microwave irradiation in 52-95% yields using benzotriazole methodology. The majority of these conjugates retain in vitro antimalarial activity with IC50 values below 100 nm, similar to quinine.

Keywords: amino acid; chemical biology; drug design; peptide.

MeSH terms

  • Antimalarials / chemical synthesis*
  • Antimalarials / pharmacology*
  • Biological Assay
  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry
  • Peptides / chemistry*
  • Quinine / chemistry*

Substances

  • Antimalarials
  • Peptides
  • Quinine