Protein‐Templated Ugi Reactions versus In‐Situ Ligation Screening: Two Roads to the Identification of SARS‐CoV‐2 Main Protease Inhibitors
Rebekka Wamser,
Xinting Zhang,
Benno Kuropka
et al.
Abstract:Protein‐templated fragment ligation was established as a method for the rapid identification of high affinity ligands, and multicomponent reactions (MCR) such as the Ugi four‐component reaction (Ugi 4CR) have been efficient in the synthesis of drug candidates. Thus, the combination of both strategies should provide a powerful approach to drug discovery. Here, we investigate protein‐templated Ugi 4CR quantitatively using a fluorescence‐based enzyme assay, HPLC‐QTOF‐MS, and native protein MS with SARS‐CoV‐2 main… Show more
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