Alkyl-linked bis-THTT derivatives as potent in vitro trypanocidal agents.
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.
Coro
Julieta
J
Laboratorio de Síntesis Orgánica, Facultad de Química, Universidad de la Habana, 10400-Ciudad Habana, Cuba.
Atherton
Richard
R
Little
Susan
S
Wharton
Hayley
H
Yardley
Vanessa
V
Alvarez
Amaury
A
Súarez
Margarita
M
Pérez
Rolando
R
Rodríguez
Hortensia
H
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
D002264:Carboxylic Acids; D013829:Thiadiazines; D014344:Trypanocidal Agents; C014846:tetrahydrothiadiazine-2-thione