Antiplasmodial activity of a series of 1,3,5-triazine-substituted polyamines.
Polyamine biosynthesis and function has been shown to be a good drug target in some parasitic protozoa and it is proposed that the pathway might also represent a target in the malaria parasite Plasmodium falciparum. A series of 1,3,5-triazine-substituted polyamine analogues were tested for activity against Plasmodium falciparum in vitro. The series showed activity against the parasites and were generally more active against the chloroquine-resistant line K1 than the chloroquine-susceptible line NF54. Simple unbranched analogues had better activity than analogues carrying branched or cyclic central chains. Addition of multiple triazine units in general led to increased activity of the compounds.
Klenke
Burkhard
B
Welsh School of Pharmacy, Cardiff University, Redwood Building, King Edward VII Avenue, Cardiff CF10 3XF, UK.
Barrett
Michael P
MP
Brun
Reto
R
Gilbert
Ian H
IH
D000818:Animals; D000962:Antimalarials / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000302:isolation & purification; D011073:Polyamines / Q000737:chemistry / Q000494:pharmacology; D014227:Triazines / Q000737:chemistry* / Q000494:pharmacology*
D000962:Antimalarials; D011073:Polyamines; D014227:Triazines; C011907:melamine