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.
Method of treating tuberculosis
申请人:Falzari Kanakeshwari
公开号:US20050014706A1
公开(公告)日:2005-01-20
Macrolide and ketolides, and compositions containing the same, useful in the treatment of tuberculosis are disclosed. Methods of treating tuberculosis using the macrolides and ketolides, and compositions containing the same, also are disclosed.