Catalytic site-selective synthesis and evaluation of a series of erythromycin analogs

The generation of a series of analogs of erythromycin A (EryA, 2) is described. In this study, we compared two peptide-based catalysts—one originally identified from a catalyst screen (5) and its enantiomer (ent-5)—for the selective functionalization of EryA. The semi-synthetic analogs were subjected to MIC evaluation with two bacterial strains and compared to unfunctionalized EryA.