Novel alkylpolyamine analogues that possess both antiparasitic and antimicrosporidial activity

A novel series of alkyl- or aralkyl-substituted polyamine analogues was synthesized containing a 3-7-3 polyamine backbone. These analogues were evaluated in vitro, and in one case in vivo, for activity as antitrypanosomal agents, and for activity against opportunistic infection caused by  Microsporidia . Compound 21 inhibits trypanosomal growth with an IC 50  as low as 31 nM, while compound 24shows promising activity in vitro against trypanosomes, and against  Microsporidia in vitro and in vivo.

The synthesis and evaluation of a series of bis(alkyl)-polyamine analogues is described. These analogues were synthesized by a facile route, and evaluated as antiparasitic agents in vitro and in vivo. Compound 20 possesses significant antitrypanosomal activity in vitro, while analogue 23 is effective against  Microsporidia  in vitro, and is curative for microsporidiosis in a murine model of infection.