Sie befinden Sich nicht im Netzwerk der Universität Paderborn. Der Zugriff auf elektronische Ressourcen ist gegebenenfalls nur via VPN oder Shibboleth (DFN-AAI) möglich. mehr Informationen...
The design and synthesis of 16-membered macrolides modified at the C-3 position are described. 3-
O-(3-Aryl-2-propenyl)leucomycin A
7 analogues showed improved in vitro antibacterial activities against clinically important pathogens.
The design and synthesis of 16-membered macrolides modified at the C-3 position are described. Starting from fully protected intermediate (
5), appropriate modifications including Heck reaction were performed to furnish 3-
O-(3-aryl-2-propenyl)leucomycin A
7 analogues (
9a–
9m). These leucomycin A
7 derivatives showed improved in vitro antibacterial activities against clinically important pathogens including erythromycin-resistant
Streptococcus pneumoniae (ERSP). SAR analysis of derivatives modified at the C-3 and C-3″ positions suggested that single modification at C-3 or C-3″ was effective for in vitro antibacterial activity.