Synthesis and antibacterial activity of 4″-O-heteroarylcarbamoyl derivatives of macrolide

A series of novel 4″-position modified macrolide derivatives has been synthesized via a facile procedure. Their in vitro antibacterial activities against constitutively erythromycin-resistant strains were evaluated. Among the derivatives tested, compound 8a which has 11,12-carbamate and 4″-O-heteroarylcarbamoyl groups was found to have potent activity against most resistant bacteria.