ChemInform Abstract: Synthesis and Antibacterial Activity of Novel 11,12‐Cyclic Carbonate Azithromycin 4′′‐O‐Carbamate Derivatives.

Abstract

Derivatives. -Starting from azithromycin a series of in 11,12-, and 4"-position modified derivatives (I) is synthesized and evaluated for their in vitro antibacterial activities. (Ic) and (Id) are the most effective derivatives against two strains of erythromycin-resistant Streptococcus pneumoniae whose resistance is encoded by the erm gene and the erm and mef genes, respectively. The results suggest that introduction of the prolonged arylalkylcarbamoyl group in 4"-position dramatically enhances the activity against aforementioned bacteria. -(MA, C.; LIU, Z.; SONG, H.; JIANG, R.; HE, F.; MA*, S.; J.