Allicin and derivates are cysteine protease inhibitors with antiparasitic activity
T Waag, C Gelhaus, J Rath, A Stich, M Leippe…
Index: Waag, Thilo; Gelhaus, Christoph; Rath, Jennifer; Stich, August; Leippe, Matthias; Schirmeister, Tanja Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 18 p. 5541 - 5543
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Citation Number: 40
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 ...
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