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Curr Opin Investig Drugs. 2010 Aug;11(8):876-83.

Diamidines for human African trypanosomiasis.

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University of North Carolina at Chapel Hill, Eshelman School of Pharmacy, Campus Box 7569, and Department of Pathology and Laboratory Medicine, Campus Box 7525, Chapel Hill, NC 27599, USA


Aromatic diamidines are potent trypanocides. Pentamidine, a diamidine, has been used for more than 60 years to treat human African trypanosomiasis (HAT); however, the drug must be administered parenterally and is active against first-stage HAT only, prior to the parasites causing neurological deterioration through invasion of the CNS. A major research effort to design novel diamidines has led to the development of orally active prodrugs and, remarkably, a new generation of compounds that can penetrate the CNS. In this review, progress in the development of diamidines for the treatment of HAT is discussed.

[Indexed for MEDLINE]

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