title: Diamidines for human African trypanosomiasis.
abstract: 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.
authors: 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
authors: Mary F
authors: MF
authors: Paine
authors: Michael Zhuo
authors: MZ
authors: Wang
authors: Claudia N
authors: CN
authors: Generaux
authors: David W
authors: DW
authors: Boykin
authors: W David
authors: WD
authors: Wilson
authors: Harry P
authors: HP
authors: De Koning
authors: Carol A
authors: CA
authors: Olson
authors: Gabriele
authors: G
authors: Pohlig
authors: Christian
authors: C
authors: Burri
authors: Reto
authors: R
authors: Brun
authors: Grace A
authors: GA
authors: Murilla
authors: John K
authors: JK
authors: Thuita
authors: Michael P
authors: MP
authors: Barrett
authors: Richard R
authors: RR
authors: Tidwell
mesh_terms: D000818:Animals; D001550:Benzamidines / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use*; D001711:Biotransformation; D001921:Brain / Q000378:metabolism; D002986:Clinical Trials as Topic; D015195:Drug Design; D004351:Drug Resistance; D006801:Humans; D010419:Pentamidine / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D011355:Prodrugs / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D014344:Trypanocidal Agents / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D014347:Trypanosoma brucei gambiense / Q000187:drug effects; D016833:Trypanosoma brucei rhodesiense / Q000187:drug effects; D014353:Trypanosomiasis, African / Q000188:drug therapy* / Q000469:parasitology
chemical_list: D001550:Benzamidines; D011355:Prodrugs; D014344:Trypanocidal Agents; D010419:Pentamidine; C458513:pafuramidine