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Curr Opin Investig Drugs. 2006 Feb;7(2):147-57.

Diamidines as antitrypanosomal, antileishmanial and antimalarial agents.

Author information

1
The Ohio State University, Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, Columbus 43210-1291, USA. werbovetz.1@osu.edu

Abstract

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.

PMID:
16499285
[Indexed for MEDLINE]

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