新型吡唑基硫醚作为组织蛋白酶 S 抑制剂的发现和 SAR 研究：第 1 部分。
Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors: part 1.
机构信息
Johnson & Johnson Pharmaceutical Research & Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
出版信息
Bioorg Med Chem Lett. 2010 Apr 1;20(7):2370-4. doi: 10.1016/j.bmcl.2010.01.108. Epub 2010 Jan 28.
PMID:20153648
Abstract
A series of pyrazole-based thioethers were prepared and found to be potent cathepsin S inhibitors. A crystal structure of 13 suggests that the thioether moiety may bind to the S3 pocket of the enzyme. Additional optimization led to the discovery of aminoethylthioethers with improved enzymatic activity and submicromolar cellular potency.
摘要
一系列基于吡唑的硫醚被制备出来，并被发现是有效的组织蛋白酶 S 抑制剂。13 的晶体结构表明，硫醚部分可能与酶的 S3 口袋结合。进一步的优化导致发现了具有改善的酶活性和亚微摩尔细胞效力的氨基乙基硫醚。
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