Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 29, Issue 15, Pages 1968-1973Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2019.05.034
Keywords
Calpain inhibition; Cysteine protease inhibition; Ketoamide; Alzheimer's Disease
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Funding
- AbbVie
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Aberrant activation of calpain has been observed in various pathophysiological disorders including neurode-generative diseases such as Alzheimer's Disease. Here we describe our efforts on ketoamide-based 1-benzyl-5-oxopyrrolidine-2-carboxamides as a novel series of highly selective calpain inhibitors mitigating the metabolic liability of carbonyl reduction. The most advanced compound from this new series, namely A-1212805 (ABT-957, Alicapistat) proceeded to clinical phase I studies.
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