Synthesis of Plasmepsin II Inhibitors – Potential Antimalarial Agents

Abstract

A new series of plasmepsin II (PM II) inhibitors has been prepared based on 4-aminopiperidine-tert-butyl-carbamate (1). These compounds might be useful as antimalarial drugs acting via a new mechanism, and therefore be less susceptible to parasite resistance now often observed with current antimalarial therapies. Some of the final compounds prepared exhibited encouraging inhibitory activity towards PM II.

Keywords

• Malaria
• Plasmepsin II
• Reductive Amination
• Suzuki Coupling