Abstract
| - The P2 transporter is a nucleoside transporter which is unique to the protozoan parasiteTrypanosoma brucei, the causative organism of Human African Trypanosomasis. The transporter has been shown to bind some structural motifs not recognized by other transporters. Inthis paper we describe the use of the melamine motif, a substrate of the P2 transporter, as apotential tool to selectively deliver polyamine analogues to the parasites. The synthesis of anumber of polyamine analogues attached to a variety of melamine analogues is described. Manyof the compounds were shown to competitively inhibit uptake of adenosine, indicating thatthey are recognized by the transporter. Some of the compounds showed good in vitro activityagainst the parasites.
|