Scaffold Modifications in Erythromycin Macrolide Antibiotics. A Chemical Minireview.

摘要: Clarithromycin and congeners are important antibacterial members of the erythromycin A 14-membered macrocyclic lactone family. The macrolide scaffold consists a multifunctional core that carries both chemically reactive non-reactive substituents sites. Two main approaches used in preparation macrolides. In semisynthesis, naturally occurring macrocycle serves as substrate for structural modifications peripheral substituents. This review is focused on non-activated positions. total synthesis approach, antibiotics constructed by convergent assembly building blocks from presynthesized substrates or prepared biogenetic engineering. assembled block structures linear chains cyclized macrolactonization metal-promoted cross-coupling reactions to afford macrolactone. Pendant glycoside residues introduced stereoselective glycosylation with donor complex. When available, short summary MIC data included presentations discussed.