Synthesis of stimuli-responsive functional dendron as a nanomedicine platform

Several strategies have been used to improve drug candidates1. In this context, the engineering of polymeric nanostructures, such as dendritic polymers, dendrimers, dendrons and micelles, has been highlighted due to the great growth of properties and great potential for drug delivery1,2. This universe encompasses stimuli-responsive and self-immolative and intelligent carriers, capable of triggering the release of bioactive agents from the carrier, such as drugs, genes and proteins, in response to specific cellular signals3. Here we report the synthesis in four steps of a new system drug delivery system, sensitive to glutathione reductase/trypanothione reductase (GSH/TR), with potential of improving pharmacokinetic properties of new drug candidates with antiparasic activity including a variety of clinically approved therapies as primaquine an antimalarial drug that has been investigated in repositioning for Chagas disease4,5. All compounds were synthesized and analyzed by 1H and 13C NMR, the yields of each step ranged from 30 to 81%.