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Precise transformations of natural products (NPs) can fine-tune their physicochemical properties while preserving inherently complex and evolutionarily optimized parent scaffolds. Here, we report an unprecedented lactone-to-lactam transformation on bilobalide, thus improving its stability and paving the way for biological exploration of previously inaccessible chemical space that is highly representative of the parent structure. This late-stage molecular editing of bilobalide enables facile access to a unique library of lactam analogues with altered pharmacology. Through phenotypic screening, we identify
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Xiaoding Jiang
Xu He
Jonathan Wong
JACS Au
University of Oxford
Chinese University of Hong Kong
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Jiang et al. (Tue,) studied this question.
www.synapsesocial.com/papers/68e60235b6db6435875956d7 — DOI: https://doi.org/10.1021/jacsau.4c00416