Studies on the synthetic procedure of a novel ketolide,cethromycin;

The Studies on Synthesis of Telithromycin and the Novel Ketolide Compounds, the Determination of Their Antibacterial Activities and the Study on Structure-activity Relationships;

A new process for preparation the ketolide antibiotic telithromycin by multistep reactions started from clarithromycin is reported.

A Brief Introduction on Macrolides Antibiotics of Novel Generation Ketolides;

The novel generation macrolide erythromycin derivatives have shown the improved pharmacokinetics profiles and the high activity against resistant strains,in which ketolides are the representative compounds,thus become the development emphasis for macrolide antibiotics.

According to the SAR study of ketolides and the bio-isostere principle,a new type of ketolide(1),bearing a C12 pyrazolinonyl moeity instead of the C11,12 cyclic carbamate group in telithromycin,was designed and synthesized starting from clarithromycin derivatives.

Telithromycin is the first member of a new family of the macrolide lincosamide streptogramin B class of antimicrobials,the ketolides.

Study on relationship between thioesterase domain and synthesis of ketolide;

Since the formation of C-3 ketone group of macrolactone ring depended on the ketoreductase (KR) domain of the sixth module of polyketide synthase that catalyzed the synthesis of 6-deoxy-erythronolide B, we could make KR6 domain inactivated or deleted by genetic engineering for ketolide biosynthesis.