ACS Medicinal Chemistry Letters p. 731 - 735 (2012)
Update date:2022-09-26
Topics:
Prime, Michael E.
Brookfield, Frederick A.
Courtney, Stephen M.
Gaines, Simon
Marston, Richard W.
Ichihara, Osamu
Li, Marie
Vaidya, Darshan
Williams, Helen
Pedret-Dunn, Anna
Reed, Laura
Schaertl, Sabine
Toledo-Sherman, Leticia
Beconi, Maria
MacDonald, Douglas
Munoz-Sanjuan, Ignacio
Dominguez, Celia
Wityak, John
A new series of potent TG2 inhibitors are reported that employ a 4-aminopiperidine core bearing an acrylamide warhead. We establish the structure-activity relationship of this new series and report on the transglutaminase selectivity and in vitro ADME properties of selected compounds. We demonstrate that the compounds do not conjugate glutathione in an in vitro setting and have superior plasma stability over our previous series.
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