Synthesis and Antibacterial Activity of 6-<i>O</i>-Arylbutynyl Ketolides with Improved Activity against Some Key Erythromycin-Resistant Pathogens
作者:Robert F. Keyes、Justin J. Carter、Erika E. Englund、Melissa M. Daly、Greg G. Stone、Angela M. Nilius、Zhenkun Ma
DOI:10.1021/jm025580k
日期:2003.5.1
A series of novel 6-O-substituted homopropargyl ketolides was synthesized and evaluated against various erythromycin-resistant pathogens. Promising in vitro antibacterial activity was demonstrated for compounds bearing this structural motif.
Regioselective Synthesis of Bifunctional Macrolides for Probing Ribosomal Binding
[GRAPHICS]Bifunctional macrolides projecting an anchor group to the right or left spatial position of the lactone ring were synthesized. The regioselectivity of the key [3 + 2] cycloaddition process was controlled by the remote cladinose group attached to the C-3 position. These conformationally constrained molecules were employed as molecular probes to study the ribosomal binding sites of bifunctional macrolide antibiotics.