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Título : Aziridine-2,3-dicarboxylate inhibitors targeting the major cysteine protease of Trypanosoma brucei as lead trypanocidal agents
Autor : Vicik, Radim
Hoerr, Verena
Glaser, Melanie
Schultheis, Martina
Hansell, Elizabeth
McKerrow, James H.
Holzgrabe, Ulrike
Caffrey, Conor R.
Ponte-Sucre, Alicia
Moll, Heidrun
Stich, August
Schirmeister, Tanja
Palabras clave : Aziridine-2,3-dicarboxylate inhibitors
cysteine protease
Trypanosoma brucei
Fecha de publicación : 23-Aug-2012
Citación : Bioorganic Medicinal Chemistry Letters;16:2753-2757, 2006.
Resumen : The protozoan parasite Trypanosoma brucei causes Human African trypanosomiasis, which is fatal if left untreated. Due to the toxicity of currently used drugs and emerging drug resistance, there is an urgent need for novel therapies. The major trypanosome papain-like cysteine protease expressed by the parasite (e.g., rhodesain in T. b. rhodesiense) is considered an important target for the development of new trypanocidal drugs. Series of aziridine-2,3-dicarboxylate-based cysteine protease inhibitors have been tested, most of them inhibiting rhodesain in the low micromolar range. Among these, only dibenzyl aziridine-2,3-dicarboxylates display trypanocidal activity being equipotent to the drug eflornithine. The Leu-Pro-containing aziridinyl tripeptides 13a–f are the most promising as they are not cytotoxic to macrophages up to concentrations of 125 mcM.
ISSN : 0968-0896
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