Alkyl-linked bis-THTT derivatives as potent in vitro trypanocidal agents

The potent in vitro anti-trypanosomal activity of alkyl-linked bis tetrahydro (2 H) 1,3,5 thiadiazine 2-thiones (THTT) I and II is reported. The effect of several alkyl-linked bis tetrahydro-(2 H)-1,3,5-thiadiazine-2-thione (bis-THTT) on Leishmania donovani, Trypanosoma brucei rhodesiense, and Plasm...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2006-03, Vol.16 (5), p.1312-1315
Hauptverfasser: Coro, Julieta, Atherton, Richard, Little, Susan, Wharton, Hayley, Yardley, Vanessa, Alvarez, Amaury, Súarez, Margarita, Pérez, Rolando, Rodríguez, Hortensia
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Sprache:eng
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Zusammenfassung:The potent in vitro anti-trypanosomal activity of alkyl-linked bis tetrahydro (2 H) 1,3,5 thiadiazine 2-thiones (THTT) I and II is reported. The effect of several alkyl-linked bis tetrahydro-(2 H)-1,3,5-thiadiazine-2-thione (bis-THTT) on Leishmania donovani, Trypanosoma brucei rhodesiense, and Plasmodium falciparum is reported. Most of the compounds exhibited a potent activity against the three parasitic strains but the best in vitro activity profiles were found against T. b. rhodesiense with IC 50 values ranging between 0.3 and 4 μM for the most active compounds.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2005.11.060