组织蛋白酶K抑制剂对骨吸收的作用。
Effect of cathepsin K inhibitors on bone resorption.
作者信息
Teno Naoki, Masuya Keiichi, Ehara Takeru, Kosaka Takatoshi, Miyake Takahiro, Irie Osamu, Hitomi Yuko, Matsuura Naoko, Umemura Ichiro, Iwasaki Genji, Fukaya Hiroaki, Toriyama Kazuhiro, Uchiyama Noriko, Nonomura Kazuhiko, Sugiyama Ikuo, Kometani Motohiko
机构信息
Novartis Institutes for BioMedical Research, Ohkubo 8, Tsukuba, Ibaraki 300-2611, Japan.
出版信息
J Med Chem. 2008 Sep 11;51(17):5459-62. doi: 10.1021/jm800626a. Epub 2008 Aug 16.
On the basis of the pyrrolopyrimidine core structure that was previously discovered, cathepsin K inhibitors having a spiro amine at the P3 have been explored to enhance the target, bone marrow, tissue distribution. Several spiro structures were identified with improved distribution toward bone marrow. The representative inhibitor 7 of this series revealed in vivo reduction in C-terminal telopeptide of type I collagen in rats and monkeys.
基于先前发现的吡咯并嘧啶核心结构，已对在P3位具有螺胺的组织蛋白酶K抑制剂进行了探索，以增强其在靶标骨髓的组织分布。已鉴定出几种对骨髓分布有所改善的螺环结构。该系列的代表性抑制剂7在大鼠和猴子体内显示出I型胶原蛋白C端端肽减少。
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