Ketones as building blocks for dynamic combinatorial libraries:: Highly active neuraminidase inhibitors generated via selection pressure of the biological target

被引：78

作者：

Hochgürtel, M ^{[1
]}

Biesinger, R ^{[1
]}

Kroth, H ^{[1
]}

Piecha, D ^{[1
]}

Hofmann, MW ^{[1
]}

Krause, S ^{[1
]}

Schaaf, O ^{[1
]}

Nicolau, C ^{[1
]}

Eliseev, AV ^{[1
]}

机构：

[1] Therascope AG, D-69120 Heidelberg, Germany

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 03期

关键词：

D O I：

10.1021/jm025589m

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

New and potent inhibitors of neuraminidase, a key enzyme in the influenza virus activity, have been discovered in dynamic combinatorial libraries based on ketones and amines as building blocks. Selective synthesis of a number of inhibitors among multiple theoretically possible combinations of building blocks is driven by the presence of the target enzyme.

引用

页码：356 / 358

页数：3