SAR Development of Lysine-Based Irreversible Inhibitors of Transglutaminase 2 for Huntington's Disease
作者
WITYAK JOHN; PRIME MICHAEL E; BROOKFIELD FREDERICK A; COURTNEY STEPHEN M; ERFAN SAYEH; JOHNSEN SIW; JOHNSON PETER D; LI MARIE; MARSTON RICHARD W; REED LAURA; VAIDYA DARSHAN; SCHAERTL SABINE; PEDRETDUNN ANNA; BECONI MARIA; MACDONALD DOUGLAS; MUNOZSANJUAN IGNACIO; DOMINGUEZ CELIA
[摘要]：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.
