engleski

The Novel Sulfonamides of 15-Membered Azalides as Inhibitors of Resistant Streptococcus pyogenes Strain

Macrolide antibiotic azithromycin 1, the first representative of the azalide class, is well-established antimicrobial agent for a treatment of respiratory tract infections.[1] Due to the unexpectedly rapid emergence of macrolide-resistant Streptococcus pneumoniae and Streptococcus pyogenes among clinical isolates, significant efforts have been devoted to the chemical modification of the existing macrolides. As part of our continuous synthetic efforts focused on a preparation of 9a-substituted azalide derivatives [2] we have recently reported the synthesis of novel sulfonylureas of 15-membered azalides which showed improved activity against inducible resistant S. pyogenes strains.[3] Those results prompted us to further explore modifications at position 9a of an azalide lacton ring, especially by the carbamoyl group linked sulfonamides, such as sulfanilamide, sulfabenz, sulfapyridine and sulfamethoxazole.

macrolide antibiotic ; macrolide-resistant Streptococcus pneumoniae ; Streptococcus pyogenes ; 9a-substituted azalide derivatives

nije evidentirano