Synthesis of exo??3??Amino??7??azabicyclo [2.2. 1] heptanes as a Class of Malarial Aspartic Protease Inhibitors: Exploration of Two Binding Pockets

M Zürcher, F Hof, L Barandun, A Schütz…

Index: Zuercher, Martina; Hof, Fraser; Barandun, Luzi; Schuetz, Andri; Schweizer, W. Bernd; Meyer, Solange; Bur, Daniel; Diederich, Francois European Journal of Organic Chemistry, 2009 , # 11 p. 1707 - 1719

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Citation Number: 4

Abstract

Abstract The increasing prevalence of drug-resistant strains of malaria-causing Plasmodium parasites necessitates the development of therapeutic agents that inhibit new biochemical targets. We herein describe the design, synthesis, and in vitro evaluation of a class of inhibitors that target the malarial aspartic proteases known as the plasmepsins. The title compounds feature a 7-azanorbornane skeleton that bears an exo-amino function, which ...