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10.1021/ml3001352

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C4025765!4025765!24900540
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suck abstract from ncbi


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pmid24900540      ACS+Med+Chem+Lett 2012 ; 3 (9): 731-5
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  • Irreversible 4-Aminopiperidine Transglutaminase 2 Inhibitors for Huntington s Disease #MMPMID24900540
  • Prime M; Brookfield FA; Courtney SM; Gaines S; Marston RW; Ichihara O; Li M; Vaidya D; Williams H; Pedret-Dunn A; Reed L; Schaertl S; Toledo-Sherman L; Beconi M; Macdonald D; Muņoz-Sanjuan I; Dominguez C; Wityak J
  • ACS Med Chem Lett 2012[Sep]; 3 (9): 731-5 PMID24900540show ga
  • 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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