Diamidines for human African trypanosomiasis

被引：0

作者：

Paine, Mary F. ^{[2
,3
]}

Wang, Michael Zhuo ^{[2
,3
]}

Generaux, Claudia N. ^{[2
,3
]}

Boykin, David W. ^{[4
]}

Wilson, W. David ^{[4
]}

De Koning, Harry P. ^{[1
]}

Olson, Carol A. ^{[5
]}

Pohlig, Gabriele ^{[6
,7
]}

Burri, Christian ^{[6
,7
]}

Brun, Reto ^{[6
,7
]}

Murilla, Grace A. ^{[8
]}

Thuita, John K. ^{[8
]}

Barrett, Michael P. ^{[1
]}

Tidwell, Richard R. ^{[2
,3
]}

机构：

[1] Univ Glasgow, Wellcome Trust Ctr Mol & Biochem Parasitol, Inst Infect Immun & Inflammat, Glasgow Biomed Res Ctr, Glasgow G12 8TA, Lanark, Scotland

[2] Univ N Carolina, Eshelman Sch Pharm, Chapel Hill, NC 27599 USA

[3] Dept Pathol & Lab Med, Chapel Hill, NC 27599 USA

[4] Georgia State Univ, Dept Chem, Atlanta, GA 30302 USA

[5] Sapphire Oak Consultants, Lindenhurst, IL 60046 USA

[6] Swiss Trop & Publ Hlth Inst, Dept Pharmaceut Med, CH-4051 Basel, Switzerland

[7] Swiss Trop & Publ Hlth Inst, Dept Med Parasitol, CH-4051 Basel, Switzerland

[8] Trypanosomiasis Res Ctr, Kenya Agr Res Inst, Kikuyu, Kenya

来源：

CURRENT OPINION IN INVESTIGATIONAL DRUGS | 2010年 / 11卷 / 08期

关键词：

Blood-brain barrier; clinical trial; diamidine; drug metabolism; drug transport; furamidine; human African trypanosomiasis; pentamidine; sleeping sickness; SUBSTRATE RECOGNITION MOTIFS; ANTIPROTOZOAL ACTIVITY; PURINE TRANSPORTER; RNA-INTERFERENCE; PRODRUG DB289; AZA-ANALOGS; BRUCEI; PENTAMIDINE; RESISTANCE; AFFINITY;

D O I：

暂无

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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.

引用

页码：876 / 883

页数：8

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