当前位置: X-MOL 学术ACS Infect. Dis. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Design and Synthesis of Broad Spectrum Trypanosomatid Selective Inhibitors
ACS Infectious Diseases ( IF 5.3 ) Pub Date : 2018-01-09 00:00:00 , DOI: 10.1021/acsinfecdis.7b00187
Andrew L. Fraser 1 , Stefanie K. Menzies 1 , Elizabeth F. B. King 1 , Lindsay B. Tulloch 1 , Eoin R. Gould 1 , Marija K. Zacharova 1 , Terry K. Smith 1 , Gordon J. Florence 1
Affiliation  

Neglected tropical diseases caused by parasitic infections are an ongoing and increasing concern that have a devastating effect on the developing world due to their burden on human and animal health. In this work, we detail the preparation of a focused library of substituted-tetrahydropyran derivatives and their evaluation as selective chemical tools for trypanosomatid inhibition and the follow-on development of photoaffinity probes capable of labeling target protein(s) in vitro. Several of these functionalized compounds maintain low micromolar activity against Trypanosoma brucei, Trypanosoma cruzi, Leishmania major, and Leishmania donovani. In addition, we demonstrate the utility of the photoaffinity probes for target identification through preliminary cellular localization studies.

中文翻译:

广谱锥虫选择性抑制剂的设计与合成

由寄生虫感染引起的被忽视的热带病是一种持续不断的关注,由于对人类和动物健康的负担,它们对发展中世界具有毁灭性影响。在这项工作中,我们详细介绍了取代的四氢吡喃衍生物的重点文库的制备及其评估,作为选择性化学工具对锥虫的抑制作用以及随后能够在体外标记靶蛋白的光亲和探针的开发。这些功能化的化合物中的几种对布鲁氏锥虫克鲁斯锥虫利什曼原虫和多形利什曼原虫保持较低的微摩尔活性。。另外,我们通过初步的细胞定位研究证明了光亲和探针对靶标鉴定的实用性。
更新日期:2018-01-09
down
wechat
bug