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

Julieta Coro; Richard Atherton; Susan Little; Hayley Wharton; Vanessa Yardley; Amaury Alvarez Jr; Margarita Súarez; Rolando Pérez; Hortensia Rodríguez

doi:10.1016/j.bmcl.2005.11.060

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. Epub 2005 Dec 15.

Authors

Julieta Coro¹, Richard Atherton, Susan Little, Hayley Wharton, Vanessa Yardley, Amaury Alvarez Jr, Margarita Súarez, Rolando Pérez, Hortensia Rodríguez

Affiliation

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Alkylation
Animals
Carboxylic Acids / chemistry
Leishmania donovani / drug effects
Molecular Structure
Plasmodium falciparum / drug effects
Structure-Activity Relationship
Thiadiazines / chemical synthesis*
Thiadiazines / chemistry
Thiadiazines / pharmacology*
Thiadiazines / toxicity
Trypanocidal Agents / chemical synthesis*
Trypanocidal Agents / chemistry
Trypanocidal Agents / pharmacology*
Trypanocidal Agents / toxicity
Trypanosoma brucei rhodesiense / drug effects

Substances

Carboxylic Acids
Thiadiazines
Trypanocidal Agents
tetrahydrothiadiazine-2-thione