Selective DYRK1A Inhibitor for the Treatment of Neurodegenerative Diseases: Alzheimer, Parkinson, Huntington, and Down Syndrome.
Basic Information
ID: ALA4725420
Journal: ACS Med Chem Lett
Title: Selective DYRK1A Inhibitor for the Treatment of Neurodegenerative Diseases: Alzheimer, Parkinson, Huntington, and Down Syndrome.
Authors: Kargbo RB
Abstract: Separation of the preferred enantiomer from racemic mixtures, i.e. "chiral switching," often improves efficacy and reduces toxicity. However, this strategy is not applicable for all chiral compounds-particularly for molecules with hydrogen-containing chiral centers, which can be prone to rapid stereoisomerization. Deuterium incorporation can stabilize such chiral centers while retaining the pharmacologic characteristics of the parent racemic mixture, thereby enabling their "chiral switching", changing the drug from a racemate to a single enantiomer. We describe "deuterium-enabled chiral switching" (DECS) as a means of improving on the therapeutic promise of chemically unstable racemic drugs and demonstrate its utility with the isolation and characterization of stable preferred enantiomers of thalidomide and thiazolidinedione (TZD) analogs.
CiteXplore: 33062155
DOI: 10.1021/acsmedchemlett.0c00346
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