In vitro anti-malarial activity of N6-modified purine analogs.
A library of N6-hydroxy-, methoxy-, or amino-adenosine analogs was prepared and screened for anti-malarial properties. We found three compounds that possess anti-plasmodial activity in the low micromolar range against the multi-drug resistant VS1 strain, namely N6-hydroxy-9H-purin-6-amine (IC50 5.57 micro M), 2-amino-N6-amino-adenosine (IC50 12.2 micro M), and 2-amino-N6-amino-N6-methyladenosine (IC50 0.29 micro M). More importantly, the compounds were non-toxic, with 2-amino-N6-amino-N6-methyladenosine showing a selectivity index of 5008.
Too
Kathleen
K
Medical Research Council, Laboratory of Molecular Biology, Cambridge, UK.
Brown
Daniel M
DM
Loakes
David
D
Bongard
Emily
E
Vivas
Livia
L
D000818:Animals; D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology*; D009584:Nitrogen / Q000737:chemistry*; D010963:Plasmodium falciparum / Q000187:drug effects*; D011687:Purines / Q000737:chemistry / Q000494:pharmacology*
D000962:Antimalarials; D011687:Purines; D009584:Nitrogen