期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 59, 期 19, 页码 9262-9268出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.6b00461
关键词
-
资金
- National Institute of Allergy and Infectious Diseases (NIAID) [AI-033066]
Two privileged fragments, caffeic acid and piperazine, were integrated into bevirimat producing new derivatives with improved activity against HIV-1/NL4-3 and NL4-3/V370A carrying the most prevalent bevirimat-resistant polymorphism. The activity of one of these, 18c, was increased by 3-fold against NL4-3 and 51-fold against NL4-3/V370A. Moreover, 18c is a maturation inhibitor with improved metabolic stability. Our study suggested that integration of privileged motifs into promising natural product skeletons is an effective strategy for discovering potent derivatives.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据