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

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 IC50 values ranging from 12 to 207 nM, similar to quinine itself. © 2012 The Royal Society of Chemistry.