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":"非洲人类锥虫病的二胺类药物。","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":"{\"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}","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}
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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