Erythromycin 9-oxime Derivatives Synthesis And In Vivo Antibacterial Activity

Erythromycin is a 14-member marcolide antibiotics which is widely used in clinic to cure diseases caused by G~+, such as respiratory infections, venereal diseases and other infections. Chemical modification of erythromycin has a history of over 50 years, in order to enhance its antibacterial activity, lots of erythromycin derivatives have been found out to be good antibiotics.Based on recent studies about chemical modification of erythromycin, we modified position 9, position 2' and position 4" on erythromycin molecular. Heterocycles including atoms such as oxygen and nitrogen were introduced to position 9, and hydoxy groups of position 2' and 4" were acylated, thus 22 new erythromycin derivatives were synthesized and their structures were confirmed by MS and ~1H-NMR.Eight representative new compounds were selected and tested in mice to evaluate their antibacterial activities. The results indicate that most of them have good antibacterial activities. Compound 14N is the best one that has better antibacterial activities than both Roxithromycin and Clarithromycin against Staphylococcus aureaus05-22, streptococcus pneumoniae 05-67 and moraxella catarrhalis05-4 etc. These new erythromycin derivatives are worthy of further research.