Benzyl prolinate derivatives as novel selective KCC2 blockers
Benzyl prolinate derivatives as novel selective KCC2 blockers
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DOI：
10.1016/j.bmcl.2010.02.092
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发表时间：
2010-04-15
影响因子：
2.7
通讯作者：
Provins, Laurent
中科院分区：
文献类型：
--
作者：
Pegurier, Cecile;Bosman, Nathalie;Provins, Laurent
描述了一类新的选择性亚微摩尔KCC2阻断剂的发现和优化。详细的合成和SAR一起给出所选化合物的ADME性质。在R（1）苯基上的甲基砜残基改善了总的一般性质。这些脯氨酸衍生物。(C)2010爱思唯尔有限公司版权所有。
The discovery and optimization of a novel class of selective submicromolar KCC2 blockers is described. Details of synthesis and SAR are given together with ADME properties of selected compounds. A methylsulfone residue on the R(1) phenyl group improved the overall general pro. le of these prolinate derivatives. (C) 2010 Elsevier Ltd. All rights reserved.