Merck Research Laboratories, MSD, Newhouse, Lanarkshire ML1 5SH, UK.
Bioorg Med Chem Lett. 2010 Aug 1;20(15):4447-50. doi: 10.1016/j.bmcl.2010.06.049. Epub 2010 Jun 15.
Starting from previously disclosed equally potent cathepsin K and S inhibitor 4-propyl-6-(3-trifluoromethylphenyl)pyrimidine-2-carbonitrile 1, a novel 2-phenyl-9H-purine-6-carbonitrile scaffold was identified to provide potent and selective cathepsin S inhibitors.
从先前公开的同样有效的组织蛋白酶 K 和 S 抑制剂 4-丙基-6-(3-三氟甲基苯基)嘧啶-2-甲腈 1 出发,鉴定出一种新型的 2-苯基-9H-嘌呤-6-甲腈骨架,以提供有效的和选择性的组织蛋白酶 S 抑制剂。