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开发治疗人类非洲锥虫病的新药。

Development of novel drugs for human African trypanosomiasis.

机构信息

Department Medical Parasitology & Infection Biology, Swiss Tropical & Public Health Institute, and, University of Basel, CH-4002 Basel, Switzerland.

出版信息

Future Microbiol. 2011 Jun;6(6):677-91. doi: 10.2217/fmb.11.44.

Abstract

Human African trypanosomiasis (HAT) or 'sleeping sickness' is a neglected tropical disease caused by the parasite Trypanosoma brucei. Novel models for funding pharmaceutical development against HAT are beginning to yield results. The Drugs for Neglected Diseases initiative (DNDi) rediscovered a nitroimidazole, fexinidazole, which is currently in Phase I clinical trials. Novel benzoxaboroles, discovered by Anacor, Scynexis and DNDi, have good pharmacokinetic properties in plasma and in the brain and are curative in a murine model of stage two HAT with brain infection. The Consortium for Parasitic Drug Development (CPDD) has identified a series of dicationic compounds that can cure a monkey model of stage two HAT. With other screening programs yielding hits, the pipeline for new HAT drugs might finally begin to fill.

摘要

人类非洲锥虫病(HAT)又称“昏睡病”,是由寄生虫布氏锥虫引起的一种被忽视的热带病。针对 HAT 的药物研发新的资助模式开始取得成果。药品专利池组织(DNDi)重新发现了一种硝基咪唑类化合物菲硝唑,目前正在进行 I 期临床试验。Anacor、Scynexis 和 DNDi 发现的新型苯并恶唑硼烷在血浆和大脑中有良好的药代动力学特性,在感染大脑的二期 HAT 小鼠模型中具有治愈作用。寄生虫药物开发联盟(CPDD)已经确定了一系列可以治愈二期 HAT 猴模型的二价化合物。随着其他筛选项目取得进展,新的 HAT 药物可能终于开始出现。

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