5,5'-bis-(4-amidinophenyl)-2,2'-bifuran derivatives and related compounds as antiprotozoal agent and prodrugs thereof

摘要

Novel dicationic bichalcophene compounds of formula (I) are described. The presently disclosed novel dicationic bichalcophene compounds exhibit in vitro activity versus Trypanosoma brucei rhodesiense, Plasmodium falciparum, or Leishmania donovani comparable to that of pentamidine and furamidine. Some of the novel dicationic bichalcophene compounds displayed good activity in vivo in a murine model of a Trypanosoma brucei rhodesiense infection.
wherein:
X 1 and X 2 are independetly selected from the group consisting of O, S, Se, Te, and NR 1 ,
Ar 1 and Ar 2 are independently selected from the group consisting of phenyl, pyridine, and benzimidazole;
Am 1 and Am 2 are each