pafuramidine and Leishmaniasis

Diamidine-containing compounds have a long history of use in the treatment of African trypanosomiasis and leishmaniasis. The discovery that diamidine prodrugs possess in vivo antimicrobial activity when administered orally has led to a renewed interest in this class of compounds for the treatment of parasitic infections. In this review, the selectivity of diamidines against trypanosomes, Leishmania and Plasmodium is rationalized through mechanism-of-action studies. An overview of the antiprotozoal activities of newer diamidines and diamidine prodrugs is also presented, along with a summary of the progress made toward the clinical development of new diamidines for use against these parasitic diseases.

Topics: Animals; Antimalarials; Antiprotozoal Agents; Benzamidines; Chagas Disease; Clinical Trials as Topic; Drug Evaluation, Preclinical; Humans; Leishmania; Leishmaniasis; Malaria, Falciparum; Pentamidine; Plasmodium falciparum; Prodrugs; Trypanocidal Agents; Trypanosoma brucei gambiense; Trypanosoma cruzi; Trypanosomiasis, African