Design, synthesis, and in vitro evaluation of potential West Nile virus protease inhibitors based on the 1-oxo-1,2,3,4-tetrahydroisoquinoline and 1-oxo-1,2-dihydroisoquinoline scaffolds.
Design, synthesis, and in vitro evaluation of potential West Nile virus protease inhibitors based on the 1-oxo-1,2,3,4-tetrahydroisoquinoline and 1-oxo-1,2-dihydroisoquinoline scaffolds.
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DOI：
10.1021/cc100091h
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发表时间：
2010-11-08
影响因子：
--
通讯作者：
Groutas, William C.
中科院分区：
文献类型：
--
作者：
Dou, Dengfeng;Viwanathan, Prasanth;Li, Yi;He, Guijia;Alliston, Kevin R.;Lushington, Gerald H.;Brown-Clay, Joshua D.;Padmanabhan, R.;Groutas, William C.
1-氧代-1，2，3，4-四氢异喹啉和1-氧代-1，2-二氢异喹啉骨架用于设计和液相合成用于筛选抗西尼罗病毒（WNV）蛋白酶的化合物的聚焦文库。探索性研究已经导致了WNV蛋白酶抑制剂（基于1-氧代-1，2-二氢异喹啉的衍生物，12 j）的鉴定，其可以潜在地用作命中-先导优化活动的发射台。鉴定的命中物对一组哺乳动物丝氨酸蛋白酶没有任何抑制活性。
The 1-Oxo-1, 2, 3, 4-tetrahydroisoquinoline and 1-Oxo-1, 2-dihydroisoquinoline scaffolds were utilized in the design and solution phase synthesis of focused libraries of compounds for screening against West Nile Virus (WNV) protease. Exploratory studies have lead to the identification of a WNV protease inhibitor (a 1-oxo-1, 2-dihydroisoquinoline-based derivative, 12j) which could potentially serve as a launching pad for a hit-to-lead optimization campaign. The identified hit was devoid of any inhibitory activity toward a panel of mammalian serine proteases.
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