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
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
Curr Opin Investig Drugs. 2010 Aug;11(8):876-83.
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.
芳香二脒是有效的杀锥虫剂。二脒类药物喷他脒已用于治疗人类非洲锥虫病（HAT）60多年；然而，该药物必须通过肠胃外给药，且仅对第一阶段的HAT有效，即在寄生虫通过侵入中枢神经系统导致神经功能恶化之前。设计新型二脒的一项重大研究工作已促成了口服活性前药的开发，并且显著地开发出了新一代能够穿透中枢神经系统的化合物。在本综述中，将讨论用于治疗HAT的二脒类药物的开发进展。
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