Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2010 Sep 15;20(18):5541-3. doi: 10.1016/j.bmcl.2010.07.062. Epub 2010 Aug 6.

Allicin and derivates are cysteine protease inhibitors with antiparasitic activity.

Author information

1
Institute of Pharmacy and Food Chemistry, University of Würzburg, Am Hubland, 97074 Würzburg, Germany.

Abstract

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.

PMID:
20692829
DOI:
10.1016/j.bmcl.2010.07.062
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center