Exploration of the P2-P3SAR of aldehyde cathepsin K inhibitors
Exploration of the P2-P3SAR of aldehyde cathepsin K inhibitors
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DOI：
10.1016/j.bmcl.2004.04.084
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发表时间：
2004-07-05
影响因子：
2.7
通讯作者：
Wright, LL
中科院分区：
文献类型：
--
作者：
Boros, EE;Deaton, DN;Wright, LL
报道了一系列组织蛋白酶K醛类抑制剂的合成及其生物活性。在P-2和P-3位取代一系列氨基甲酸酯衍生的正亮氨酸醛，探索S-2和S-3亚位点的性质，得到组织蛋白酶K IC（50）在600 nM和130 pM之间的类似物。(C)2004爱思唯尔有限公司保留所有权利。
The synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S-2 and S-3 subsites with a series of carbamate derivatized norleucine aldehydes substituted at the P-2 and P-3 positions afforded analogs with cathepsin K IC(50)s between 600 nM and 130 pM. (C) 2004 Elsevier Ltd. All rights reserved.