title: Alkyl-linked bis-THTT derivatives as potent in vitro trypanocidal agents.
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.
authors.affiliation: Laboratorio de Síntesis Orgánica, Facultad de Química, Universidad de la Habana, 10400-Ciudad Habana, Cuba.
authors.forename: Julieta
authors.initials: J
authors.lastname: Coro
authors.forename: Richard
authors.initials: R
authors.lastname: Atherton
authors.forename: Susan
authors.initials: S
authors.lastname: Little
authors.forename: Hayley
authors.initials: H
authors.lastname: Wharton
authors.forename: Vanessa
authors.initials: V
authors.lastname: Yardley
authors.forename: Amaury
authors.initials: A
authors.lastname: Alvarez
authors.forename: Margarita
authors.initials: M
authors.lastname: Súarez
authors.forename: Rolando
authors.initials: R
authors.lastname: Pérez
authors.forename: Hortensia
authors.initials: H
authors.lastname: Rodríguez
mesh_terms: D000478:Alkylation; D000818:Animals; D002264:Carboxylic Acids / Q000737:chemistry; D007893:Leishmania donovani / Q000187:drug effects; D015394:Molecular Structure; D010963:Plasmodium falciparum / Q000187:drug effects; D013329:Structure-Activity Relationship; D013829:Thiadiazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D016833:Trypanosoma brucei rhodesiense / Q000187:drug effects
chemical_list: D002264:Carboxylic Acids; D013829:Thiadiazines; D014344:Trypanocidal Agents; C014846:tetrahydrothiadiazine-2-thione