Mary F Paine, Michael Zhuo Wang, Claudia N Generaux, David W Boykin, W David Wilson, Harry P De Koning, Carol A Olson, Gabriele Pohlig, Christian Burri, Reto Brun, Grace A Murilla, John K Thuita, Michael P Barrett, Richard R Tidwell
{"title":"Diamidines for human African trypanosomiasis.","authors":"Mary F Paine, Michael Zhuo Wang, Claudia N Generaux, David W Boykin, W David Wilson, Harry P De Koning, Carol A Olson, Gabriele Pohlig, Christian Burri, Reto Brun, Grace A Murilla, John K Thuita, Michael P Barrett, Richard R Tidwell","doi":"","DOIUrl":null,"url":null,"abstract":"<p><p>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.</p>","PeriodicalId":10978,"journal":{"name":"Current opinion in investigational drugs","volume":"11 8","pages":"876-83"},"PeriodicalIF":0.0000,"publicationDate":"2010-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current opinion in investigational drugs","FirstCategoryId":"1085","ListUrlMain":"","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0
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.
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