人破骨细胞组织蛋白酶K的二氨基吡咯烷酮抑制剂的设计与合成
Design and synthesis of diaminopyrrolidinone inhibitors of human osteoclast cathepsin K.
作者信息
Duffy K J, Ridgers L H, DesJarlais R L, Tomaszek T A, Bossard M J, Thompson S K, Keenan R M, Veber D F
机构信息
Department of Medicinal Chemistry, SmithKline Beecham Pharmaceuticals, Collegeville, PA 19246, USA.
出版信息
Bioorg Med Chem Lett. 1999 Jul 19;9(14):1907-10. doi: 10.1016/s0960-894x(99)00322-4.
Abstract
The structure-based design and synthesis of lactam-constrained azapeptide inhibitors of human cathepsin K are described. Enhanced stability to proteolytic cleavage over acyclic analogues is discussed.
摘要
本文描述了基于结构的人组织蛋白酶K的内酰胺约束氮杂肽抑制剂的设计与合成。文中讨论了相较于无环类似物，其对蛋白水解切割的稳定性增强。
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