1251465-28-7Relevant articles and documents
Irreversible 4-aminopiperidine transglutaminase 2 inhibitors for Huntington's disease
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
, p. 731 - 735 (2012)
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.
ANTIVIRAL PYRIMIDINES
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Page/Page column 114, (2010/11/03)
Disclosed herein are novel compounds comprising substituted pyrimidines, pyrazolopyrimtdines, and imidazolopyrimidines, the syntheses thereof, and compositions thereof, including pharmaceutical compositions, comprising the novel pyrimidines, pyrazolopyrimtdines, imidazolpyrimidines and related compounds. Such compounds function to inhibit entry of viruses of the Flaviviridae family, including Hepatitis C virus (HCV), into cells that are susceptible to virus infection. These compounds are useful for the treatment, therapy and/or prophylaxis of viral diseases and infection, including HCV infection.