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alpha-Ketoheterocycles as inhibitors of leishmania mexicana cysteine protease CPB

Steert, Koen and Berg, Maya and Mottram, Jeremy C. and Westrop, Gareth D. and Coombs, Graham H. and Cos, Paul and Maes, Louis and Joossens, Jurgen and Van der Veken, Pieter and Haemers, Achiel and Augustyns, Koen (2010) alpha-Ketoheterocycles as inhibitors of leishmania mexicana cysteine protease CPB. ChemMedChem, 5 (10). pp. 1734-1748. ISSN 1860-7179

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Abstract

Cysteine proteases of the papain superfamily are present in nearly all eukaryotes and also play pivotal roles in the biology of parasites. Inhibition of cysteine proteases is emerging as an important strategy to combat parasitic diseases such as sleeping sickness, Chagas disease, and leishmaniasis. Inspired by the in vivo antiparasitic activity of the vinylsulfone-based cysteine protease inhibitors, a series of alpha-ketoheterocycles were developed as reversible inhibitors of a recombinant L. mexicana cysteine protease, CPB2.8. Three isoxazoles and especially one oxadiazole compound are potent reversible inhibitors of CPB2.8; however, in vitro whole-organism screening against a panel of protozoan parasites did not fully correlate with the observed inhibition of the cysteine protease.