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26 février 2011 6 26 /02 /février /2011 10:39

Bioorg Med Chem Lett. 2010 Sep 15;20(18):5541-3. Epub 2010 Aug 6.

Allicin and derivates are cysteine protease inhibitors with antiparasitic activity.

Waag TGelhaus CRath JStich ALeippe MSchirmeister T.

Institute of Pharmacy and Food Chemistry, University of Würzburg, Am Hubland, 97074 Würzburg, Germany.

Allicin and derivatives thereof inhibit the CAC1 cysteine proteases falcipain 2, rhodesain, cathepsin B and L in the low micromolar range. The structure-activity relationship revealed that only derivatives with primary carbon atom in vicinity to the thiosulfinate sulfur atom attacked by the active-site Cys residue are active against the target enzymes.

Some compounds also show potent antiparasitic activity against Plasmodium falciparum and Trypanosoma brucei brucei.

Copyright (c) 2010 Elsevier Ltd. All rights reserved.

PMID: 20692829 [PubMed - indexed for MEDLINE]

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