Abstract Puromycin derivatives containing an emissive thieno[3,4‐d]‐pyrimidine core, modified with azetidine and 3,3‐difluoroazetidine as Me2N surrogates, exhibit translation inhibition and bactericidal activity similar to the natural antibiotic. The analogues are capable of cellular puromycylation of nascent peptides, generating emissive products without any follow‐up chemistry. The 3,3‐difluoroazetidine‐containing analogue is shown to fluorescently label newly translated peptides and be visualized in both live and fixed HEK293T cells and rat hippocampal neurons.
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