The promising in vitro and in vivo activities of dicationic molecules clearly indicate that aromatic diamidines are the most promising class of compounds for the development of newer drugs against HAT. The most important one is the newer analogous of existing drugs pentamidine (compounds 32, Figure 3e and 66, Figure 3b ) which shows excellent in vivo and in vitro activity (0.004 and 0.001 μM respectively) and also has very good selectivity index against the parasite but is cytotoxic. In an attempt to synthesise newer compounds with reduced cytotoxicity than pentamidine molecules, several benzofuran derivatives have been synthesized. However the replacement of phenoxy fragement of pentamidine with a benzofuran motif has resulted in poor analogues with lower antitrypanosomal activity but improved cytotoxic profile. However the strong activity against T. b. rhodesiense isolates indicates that steps should be taken to initiate further studies of compound 66 and compound 32 which can be further evolved as new lead compound. The newer analogues of furamidine also show promising anti-trypanosomal activity along with lower cytotoxicity than furamidine. Thus strong activity against T. b. rhodesiense and lower cytotoxicity of compound 3 (Figure 13b ) indicates that these compounds should be further evaluated. Thus the DNA minor grove binders are still the most interesting and potential target for the development of newer anti-trypanosomal agents.