Pentamidine, furamidine and its analogues lack oral bioavailability [82, 83] .In addition several analogues of furamidine show excellent activity on intravenous dosing but are ineffective on oral administration [83, 84] . Generally, oral administration is the preferred dosing regime, and hence, prodrug strategies for diamidines that have the potential to overcome their limited oral bioavailability merit attention. The following works have been performed by Boykin DW et al to develop prodrugs.