Diamidines for human African trypanosomiasis

作者：Paine Mary F; Wang Michael Zhuo; Generaux Claudia N; Boykin David W; Wilson W David; De Koning Harry P; Olson Carol A; Pohlig Gabriele; Burri Christian; Brun Reto; Murilla Grace A; Thuita John K; Barrett Michael P^*; Tidwell Richard R

来源：Current Opinion in Investigational Drugs, 2010, 11(8): 876-883.

• Blood-brain barrier
• clinical trial
• diamidine
• drug metabolism
• drug transport
• furamidine
• human African trypanosomiasis
• pentamidine
• sleeping sickness

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.

• 出版日期2010-8