Stereospecific synthesis of chiral 2,3-dihydro-1,4-benzodithiine and methyl-2,3-dihydro-1,4-benzodithiine derivatives and their toxic effects on Trypanosoma brucei |
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Authors: | Ali Shah Syed Tasadaque Merkel Patrick Ragge Hubert Duszenko Michael Rademann Jörg Voelter Wolfgang |
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Affiliation: | Physiologisch-chemisches Institut der Universit?t Tübingen, Hoppe-Seyler Strasse 4, 72076 Tübingen, Germany. |
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Abstract: | Preparation of chiral 2,3-dihydro-1,4-benzodithiine and methyl-2,3-dihydro-1,4-benzodithiine derivatives with known absolute configurations from the easily accessible chiral synthons benzyl 4-O-trifloxy-2,3-anhydro-beta-L-ribopyranoside and benzyl 4-O-trifloxy-2,3-anhydro-alpha-D-ribopyranoside is described. These compounds showed significant in vitro toxicity of the bloodstream form of Trypanosoma brucei with an IC50 of 11 microM. The parasites' energy metabolism and consumption of oxygen were found to be affected during incubation. |
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Keywords: | antibiotics benzodithiine oxidases sugars Trypanosoma brucei |
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