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

Julieta Coro; Richard Atherton; Susan Little; Hayley Wharton; Vanessa Yardley; Amaury Alvarez; Margarita Súarez; Rolando Pérez; Hortensia Rodríguez; (2006) Alkyl-linked bis-THTT derivatives as potent in vitro trypanocidal agents. Bioorganic & medicinal chemistry letters, 16 (5). pp. 1312-1315. ISSN 0960-894X DOI: 10.1016/j.bmcl.2005.11.060
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The effect of several alkyl-linked bis tetrahydro-(2H)-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 microM for the most active compounds.

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