✦ LIBER ✦

Allicin and derivates are cysteine protease inhibitors with antiparasitic activity

✍ Scribed by Thilo Waag; Christoph Gelhaus; Jennifer Rath; August Stich; Matthias Leippe; Tanja Schirmeister

Book ID: 104004667
Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 364 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.07.062

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✦ Synopsis

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.

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