Anti-Malarial activity of N6-Substituted adenosine derivatives. Part I Original Research Article

The synthesis and biological evaluation of novel N6-substituted adenosine derivatives is reported. The first series of compounds was obtained using an established procedure for the nucleophilic substitution of a 1-(6-chloro-purin-9-yl)-β-d-1-deoxy-ribofuranose with various amines. In addition, attachment of two different amino-functionalised spacer arms at the N6-position of adenosine enabled derivatisation by an innovative polymer-assisted protocol. Thus, we were able to prepare three series of substituted derivatives that displayed activity versus the multiresistant Plasmodium falciparum strain Dd2 in cell culture experiments.