Synthesis and Antibacterial Activity of Acylides (3-O-Acyl-erythromycin Derivatives):  A Novel Class of Macrolide Antibiotics

Introduction of an acyl group to the 3-O-position of erythromycin A derivatives instead of l-cladinose led to a novel class of macrolide antibiotics that we named “acylides”. The 3-O-nitrophenylacetyl derivative TEA0777 showed significantly potent activity against not only erythromycin-susceptible Gram-positive pathogens but also inducibly macrolides-lincosamides-streptogramin B (MLSB)-resistant Staphylococcus aureus and efflux-resistant Streptococcus pneumoniae. These results indicated that acylides have potential as next-generation macrolide antibiotics.