Grice Cheryl A, Tays Kevin, Khatuya Haripada, Gustin Darin J, Butler Christopher R, Wei Jianmei, Sehon Clark A, Sun Siquan, Gu Yin, Jiang Wen, Thurmond Robin L, Karlsson Lars, Edwards James P
Johnson and Johnson Pharmaceutical Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
Bioorg Med Chem Lett. 2006 Apr 15;16(8):2209-12. doi: 10.1016/j.bmcl.2006.01.038. Epub 2006 Feb 3.
A series of competitive, reversible cathepsin S (CatS) inhibitors was investigated. An earlier disclosure detailed the discovery of the 4-(2-keto-1-benzimidazolinyl)-piperidin-1-yl moiety as an effective replacement for the 4-arylpiperazin-1-yl group found in our screening hit. Continued investigation into replacements for the 4-aryl piperazine resulted in the identification of potentially useful CatS inhibitors with enzymatic and cellular activity similar to that of JNJ 10329670 as disclosed in a previous publication.
对一系列竞争性、可逆性组织蛋白酶S（CatS）抑制剂进行了研究。较早的一份披露详细介绍了发现4-(2-酮-1-苯并咪唑啉基)-哌啶-1-基部分可有效替代我们筛选命中物中发现的4-芳基哌嗪-1-基基团。对4-芳基哌嗪替代物的持续研究导致鉴定出具有与先前出版物中披露的JNJ 10329670相似的酶活性和细胞活性的潜在有用的CatS抑制剂。
