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ACS Med Chem Lett. 2012 Aug 9;3(9):731-5. doi: 10.1021/ml3001352. eCollection 2012 Sep 13.

Irreversible 4-Aminopiperidine Transglutaminase 2 Inhibitors for Huntington's Disease.

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Evotec (U.K.) Ltd. , 114 Milton Park, Abingdon OX14 4SA, United Kingdom.
Evotec AG , Manfred Eigen Campus, Essener Bogen 7, 22419 Hamburg, Germany.
CHDI Management/CHDI Foundation , 6080 Center Drive, Suite 100, Los Angeles, California 90045, United States.


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.


ADME; Celiac disease; SAR; acrylamides; computer-aided drug design; plasma stability

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