组织蛋白酶K抑制剂的新型支架
Novel scaffold for cathepsin K inhibitors.
作者信息
Teno Naoki, Miyake Takahiro, Ehara Takeru, Irie Osamu, Sakaki Junichi, Ohmori Osamu, Gunji Hiroki, Matsuura Naoko, Masuya Keiichi, Hitomi Yuko, Nonomura Kazuhiko, Horiuchi Miyuki, Gohda Keigo, Iwasaki Atsuko, Umemura Ichiro, Tada Sachiyo, Kometani Motohiko, Iwasaki Genji, Cowan-Jacob Sandra W, Missbach Martin, Lattmann René, Betschart Claudia
机构信息
Novartis Institutes for BioMedical Research, Ohkubo 8, Tsukuba, Ibaraki, Japan.
出版信息
Bioorg Med Chem Lett. 2007 Nov 15;17(22):6096-100. doi: 10.1016/j.bmcl.2007.09.047. Epub 2007 Sep 15.
Pyrrolopyrimidine, a novel scaffold, allows to adjust interactions within the S3 subsite of cathepsin K. The core intermediate 10 facilitated the P3 optimization and identified highly potent and selective cathepsin K inhibitors 11-20.
吡咯并嘧啶是一种新型骨架，可用于调节组织蛋白酶K的S3亚位点内的相互作用。核心中间体10促进了P3优化，并确定了高效且具有选择性的组织蛋白酶K抑制剂11 - 20。
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