Publication
Title
-ketoheterocycles as inhibitors of **Leishmania mexicana** cysteine protease CPB
Author
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 α-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.
Language
English
Source (journal)
ChemMedChem. - Place of publication unknown
Publication
Place of publication unknown : 2010
ISSN
1860-7179 [print]
1860-7187 [online]
Volume/pages
5:10(2010), p. 1734-1748
ISI
000283670200015
Full text (Publisher's DOI)
UAntwerpen
Faculty/Department
Research group
Publication type
Subject
Affiliation
Publications with a UAntwerp address
External links
Web of Science
Record
Identification
Creation 30.08.2010
Last edited 14.07.2017
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