芳基氨基乙酰胺作为组织蛋白酶S非共价抑制剂的设计与合成。第1部分。
Design and synthesis of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 1.
作者信息
Liu Hong, Tully David C, Epple Robert, Bursulaya Badry, Li Jun, Harris Jennifer L, Williams Jennifer A, Russo Ross, Tumanut Christine, Roberts Michael J, Alper Phil B, He Yun, Karanewsky Donald S
机构信息
Genomics Institute of the Novartis Research Foundation, 10675 John J. Hopkins Dr., San Diego, CA 92121, USA.
出版信息
Bioorg Med Chem Lett. 2005 Nov 15;15(22):4979-84. doi: 10.1016/j.bmcl.2005.08.017. Epub 2005 Sep 23.
A series of Nalpha-acyl-alpha-amino acid-(arylaminoethyl)amides were found to be potent and noncovalent cathepsin S inhibitors. Compound 20 possessed high cathepsin S affinity (Ki=3.3 nM) and showed excellent selectivity over cathepsin K, L, F, and V. Molecular modeling, design, synthesis, and in vitro activity are described.
一系列Nα-酰基-α-氨基酸-（芳基氨基乙基）酰胺被发现是有效的非共价组织蛋白酶S抑制剂。化合物20对组织蛋白酶S具有高亲和力（Ki = 3.3 nM），并且对组织蛋白酶K、L、F和V表现出优异的选择性。本文描述了分子建模、设计、合成及体外活性。
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