一类新型基于琥珀腈的组织蛋白酶S抑制剂的鉴定。
Identification of a novel class of succinyl-nitrile-based Cathepsin S inhibitors.
作者信息
Bekkali Younes, Thomson David S, Betageri Raj, Emmanuel Michel J, Hao Ming-Hong, Hickey Eugene, Liu Weimin, Patel Usha, Ward Yancey D, Young Erick R R, Nelson Richard, Kukulka Alison, Brown Maryanne L, Crane Kathy, White Della, Freeman Dorothy M, Labadia Mark E, Wildeson Jessi, Spero Denice M
机构信息
Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals Inc., 900 Ridgebury Road, PO Box 368, Ridgefield, CT 06877-0368, USA.
出版信息
Bioorg Med Chem Lett. 2007 May 1;17(9):2465-9. doi: 10.1016/j.bmcl.2007.02.046. Epub 2007 Feb 23.
The synthesis and in vitro activities of a series of succinyl-nitrile-based inhibitors of Cathepsin S are described. Several members of this class show nanomolar inhibition of the target enzyme as well as cellular potency. The inhibitors displaying the greatest potency contain N-alkyl substituted piperidine and pyrrolidine rings spiro-fused to the alpha-carbon of the P1 residue.
描述了一系列基于琥珀腈的组织蛋白酶S抑制剂的合成及其体外活性。该类化合物中的几个成员对目标酶表现出纳摩尔级别的抑制作用以及细胞活性。活性最强的抑制剂含有与P1残基的α-碳螺稠合的N-烷基取代哌啶和吡咯烷环。
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