Improved inhibitors of trypanothione reductase by combination of motifs: synthesis, inhibitory potency, binding mode, and antiprotozoal activities

…, R Brun, RL Krauth??Siegel, F Diederich

Index: Eberle, Christian; Lauber, Birgit Sophia; Fankhauser, Daniel; Kaiser, Marcel; Brun, Reto; Krauth-Siegel, R. Luise; Diederich, Francois ChemMedChem, 2011 , vol. 6, # 2 p. 292 - 301

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Citation Number: 16

Abstract

Abstract Trypanothione reductase (TR) is an essential enzyme in the trypanothione-based redox metabolism of trypanosomatid parasites. This system is absent in humans and, therefore, offers a promising target for the development of selective new drugs against African sleeping sickness and Chagas' disease. Over the past two decades, a variety of nonpeptidic small-molecule ligands of the parasitic enzyme were discovered. A current ...