通过骨架跳跃鉴定出的盘尾丝虫蜕皮抑制剂。
Onchocerca volvulus Molting Inhibitors Identified through Scaffold Hopping.
作者信息
Gooyit Major, Harris Tyler L, Tricoche Nancy, Javor Sacha, Lustigman Sara, Janda Kim D
机构信息
Departments of Chemistry and Immunology and Microbial Science, The Skaggs Institute for Chemical Biology, and The Worm Institute of Research and Medicine, The Scripps Research Institute , 10550 North Torrey Pines Road, La Jolla, California 92037, United States.
Lindsley F. Kimball Research Institute, New York Blood Center , New York, New York 10065, United States.
出版信息
ACS Infect Dis. 2015 May 8;1(5):198-202. doi: 10.1021/acsinfecdis.5b00017. Epub 2015 Mar 18.
The anthelmintic closantel has shown promise in abrogating the L3 molting of Onchocerca volvulus, the causative agent of the infectious disease onchocerciasis. In our search for alternative scaffolds, we utilized a fragment replacement/modification approach to generate novel chemotypes with improved chitinase inhibitory properties. Further evaluation of the compounds unveiled the potential of urea-tropolones as potent inhibitors of O. volvulus L3 molting.
驱虫药氯氰碘柳胺在阻止盘尾丝虫病的病原体盘尾丝虫的L3期蜕皮方面已显示出前景。在我们寻找替代骨架的过程中，我们采用了片段替换/修饰方法来生成具有改善的几丁质酶抑制特性的新型化学类型。对这些化合物的进一步评估揭示了尿素-托酚酮作为盘尾丝虫L3期蜕皮的有效抑制剂的潜力。
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