Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 18, Pages 5541-5543Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.07.062
Keywords
Allicin; Thiosulfinate; Cysteine protease; Inhibitor; Parasite
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Funding
- Deutsche Forschungsgemeinschaft (DFG) [SFB630]
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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. (C) 2010 Elsevier Ltd. All rights reserved.
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