SAR Development of Lysine-Based Irreversible Inhibitors of Transglutaminase 2 for Huntington's Disease
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- 作者：John Wityak ; Michael E. Prime ; Frederick A. Brookfield ; Stephen M. Courtney ; Sayeh Erfan ; Siw Johnsen ; Peter D. Johnson ; Marie Li ; Richard W. Marston ; Laura Reed ; Darshan Vaidya ; Sabine Schaertl ; Anna Pedret-Dunn ; Maria Beconi ; Douglas Macdonald ; Ignacio Mu帽oz-Sanjuan ; Celia Dominguez
- 刊名：ACS Medicinal Chemistry Letters
- 出版年：2012
- 出版时间：December 13, 2012
- 年：2012
- 卷：3
- 期：12
- 页码：1024-1028
- 全文大小：257K
- 年卷期：v.3,no.12(December 13, 2012)
- ISSN：1948-5875
文摘
We report a series of irreversible transglutaminase 2 inhibitors starting from a known lysine dipeptide bearing an acrylamide warhead. We established new SARs resulting in compounds demonstrating improved potency and better physical and calculated properties. Transglutaminase selectivity profiling and in vitro ADME properties of selected compounds are also reported.