氨基乙基氨基甲酸酯作为一类新型强效且选择性的组织蛋白酶S抑制剂。
Arylaminoethyl carbamates as a novel series of potent and selective cathepsin S inhibitors.
作者信息
Tully David C, Liu Hong, Chatterjee Arnab K, Alper Phil B, Williams Jennifer A, Roberts Michael J, Mutnick Daniel, Woodmansee David H, Hollenbeck Thomas, Gordon Perry, Chang Jonathan, Tuntland Tove, Tumanut Christine, Li Jun, Harris Jennifer L, Karanewsky Donald S
机构信息
Genomics Institute of the Novartis Research Foundation, 10675 John J. Hopkins Dr., San Diego, CA 92121, USA.
出版信息
Bioorg Med Chem Lett. 2006 Oct 1;16(19):5107-11. doi: 10.1016/j.bmcl.2006.07.032. Epub 2006 Jul 28.
We report a novel series of noncovalent inhibitors of cathepsin S. The synthesis of the peptidomimetic scaffold is described and structure-activity relationships of P3, P1, and P1' subunits are discussed. Lead optimization to a non-peptidic scaffold has resulted in a new class of potent, highly selective, and orally bioavailable cathepsin S inhibitors.
我们报道了一系列新型组织蛋白酶S的非共价抑制剂。描述了拟肽支架的合成，并讨论了P3、P1和P1'亚基的构效关系。将先导化合物优化为非肽支架已产生了一类新型的强效、高选择性且口服生物可利用的组织蛋白酶S抑制剂。
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