Onchocerca volvulus Molting Inhibitors Identified through Scaffold Hopping
详细信息 查看全文
- 作者：Major Gooyit ; Tyler L. Harris ; Nancy Tricoche ; Sacha Javor ; Sara Lustigman ; Kim D. Janda
- 刊名：ACS Infectious Diseases
- 出版年：2015
- 出版时间：May 8, 2015
- 年：2015
- 卷：1
- 期：5
- 页码：198-202
- 全文大小：280K
- ISSN：2373-8227
文摘
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.