Title
<tex>$\_alpha$</tex>-ketoheterocycles as inhibitors of **Leishmania mexicana** cysteine protease CPB <tex>$\_alpha$</tex>-ketoheterocycles as inhibitors of **Leishmania mexicana** cysteine protease CPB
Author
Faculty/Department
Faculty of Pharmaceutical, Biomedical and Veterinary Sciences. Pharmacy
Publication type
article
Publication
,
Subject
Pharmacology. Therapy
Source (journal)
ChemMedChem. - Place of publication unknown
Volume/pages
5(2010) :10 , p. 1734-1748
ISSN
1860-7179
1860-7187
ISI
000283670200015
Carrier
E
Target language
English (eng)
Full text (Publishers DOI)
Affiliation
University of Antwerp
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&#8197;vivo antiparasitic activity of the vinylsulfone-based cysteine protease inhibitors, a series of α-ketoheterocycles were developed as reversible inhibitors of a recombinant L.&#8197;mexicana cysteine protease, CPB2.8. Three isoxazoles and especially one oxadiazole compound are potent reversible inhibitors of CPB2.8; however, in&#8197;vitro whole-organism screening against a panel of protozoan parasites did not fully correlate with the observed inhibition of the cysteine protease.
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