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 μM), 2-amino-N6-amino-adenosine (IC50 12.2 μM), and 2-amino-N6-amino-N6- methyladenosine (IC50 0.29 μM). More importantly, the compounds were non-toxic, with 2-amino-N6-amino-N6-methyladenosine showing a selectivity index of 5008. Copyright © Taylor & Francis Group, LLC.