醛基组织蛋白酶K抑制剂的P1构效关系探索。
Exploration of the P1 SAR of aldehyde cathepsin K inhibitors.
作者信息
Catalano John G, Deaton David N, Furfine Eric S, Hassell Annie M, McFadyen Robert B, Miller Aaron B, Miller Larry R, Shewchuk Lisa M, Willard Derril H, Wright Lois L
机构信息
Department of Medicinal Chemistry, GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA.
出版信息
Bioorg Med Chem Lett. 2004 Jan 5;14(1):275-8. doi: 10.1016/j.bmcl.2003.09.088.
The synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S(1) subsite with a series of alpha-amino aldehyde derivatives substituted at the P(1) position afforded compounds with cathepsin K IC(50)s between 52 microM and 15 nM.
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。用一系列在P(1)位被取代的α-氨基醛衍生物对S(1)亚位点的性质进行探索，得到了组织蛋白酶K半数抑制浓度（IC(50)）在52微摩尔至15纳摩尔之间的化合物。
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