基于吡唑的芳基炔基组织蛋白酶 S 抑制剂。第三部分：P4 区域的修饰。
Pyrazole-based arylalkyne cathepsin S inhibitors. Part III: modification of P4 region.
机构信息
Janssen Research & Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
出版信息
Bioorg Med Chem Lett. 2013 Feb 15;23(4):1070-4. doi: 10.1016/j.bmcl.2012.12.014. Epub 2012 Dec 21.
Novel classes of tetrahydropyrido-pyrazole thioether amines and arylalkynes that display potency against human Cathepsin S have been previously reported. Here, key pharmacophoric elements of these two classes are merged, and SAR investigations of the P4 region are described, in conjunction with re-optimization of the P5 and P1/P1'/P3 regions. Identification of meta-substituted arylalkynes with good potency and improved solubility is described.
先前曾报道过具有抗人组织蛋白酶 S 活性的新型四氢吡啶并吡唑硫醚胺类和芳基炔类化合物。在此，将这两类化合物的关键药效团元素进行融合，并对 P4 区域进行 SAR 研究，同时对 P5 和 P1/P1'/P3 区域进行重新优化。描述了具有良好活性和改善溶解性的间位取代芳基炔的鉴定。
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