A library of novel hydroxamic acids targeting the metallo-protease family: Design, parallel synthesis and screening
A library of novel hydroxamic acids targeting the metallo-protease family: Design, parallel synthesis and screening
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DOI：
10.1016/j.bmc.2006.10.010
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发表时间：
2007-01-01
影响因子：
3.5
通讯作者：
Deprez-Poulain, Rebecca F.
中科院分区：
文献类型：
--
作者：
Flipo, Marion;Beghyn, Terence;Deprez-Poulain, Rebecca F.
我们在这里报告的设计和平行合成的217个化合物的基础上的丙二酸异羟肟酸模板。这些化合物通过两步溶液相方法获得。所使用的一组不同的构建模块使得该策略适合于搜索各种金属蛋白酶的抑制剂和用于调查新的金属蛋白酶的生物学作用。作为概念证明，我们在中性氨肽酶（APN; EC 3.4.11.2）上筛选该文库，中性氨肽酶是M1家族的原型酶。鉴定了几种亚微摩尔抑制剂。(c)2006爱思唯尔有限公司保留所有权利。
We report here the design and parallel synthesis of 217 compounds based on a malonic-hydroxamic acid template. These compounds are obtained via a two-step solution-phase procedure. The set of diverse building-blocks used makes this strategy suitable for the search of inhibitors of various metallo-proteases and for the investigation of the biological role of new metallo-proteases. As a proof of concept, we screened this library on Neutral Aminopeptidase (APN; EC 3.4.11.2), the prototypal enzyme of the M1 family. Several submicromolar inhibitors were identified. (c) 2006 Elsevier Ltd. All rights reserved.