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

  • Bioorg Med Chem Lett. 2006 Mar 1;16(5):1312-5. doi: 10.1016/j.bmcl.2005.11.060.
Julieta Coro  1 ,  Richard Atherton ,  Susan Little ,  Hayley Wharton ,  Vanessa Yardley ,  Amaury Alvarez Jr ,  Margarita Súarez ,  Rolando Pérez ,  Hortensia Rodríguez
Affiliations
  • 1. Laboratorio de Síntesis Orgánica, Facultad de Química, Universidad de la Habana, 10400-Ciudad Habana, Cuba.
PMID: 16343898 DOI: 10.1016/j.bmcl.2005.11.060
Abstract

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.