A novel ketolide class: Synthesis and antibacterial activity of a lead compound

Daniele Andreotti; Ilaria Bientinesi; Stefano Biondi; Daniele Donati; Isabelle Erbetti; Sergio Lociuro; Carla Marchioro; Alfonso Pozzan; Emiliangelo Ratti; Silvia Terreni

doi:10.1016/j.bmcl.2007.02.019

A novel ketolide class: Synthesis and antibacterial activity of a lead compound

Bioorg Med Chem Lett. 2007 Sep 15;17(18):5265-9. doi: 10.1016/j.bmcl.2007.02.019. Epub 2007 Feb 9.

Authors

Daniele Andreotti¹, Ilaria Bientinesi, Stefano Biondi, Daniele Donati, Isabelle Erbetti, Sergio Lociuro, Carla Marchioro, Alfonso Pozzan, Emiliangelo Ratti, Silvia Terreni

Affiliation

¹ GlaxoSmithKline, Medicine Research Centre, Via A Fleming 4, I-37135 Verona, Italy. [email protected]

PMID: 17681467
DOI: 10.1016/j.bmcl.2007.02.019

Abstract

Synthesis and antibacterial activity of a new class of ketolide antibiotics, exemplified by the prototype GW680788X (1), are described. The structure of (1) has been elucidated by spectroscopic analysis. The good antibacterial activity shown by (1) in comparison with clarithromycin prompted us to consider this compound as a lead molecule for further exploration.

MeSH terms

Anti-Bacterial Agents / chemical synthesis*
Anti-Bacterial Agents / pharmacology*
Ketolides / chemical synthesis*
Ketolides / pharmacology*
Microbial Sensitivity Tests
Models, Molecular

Substances

Anti-Bacterial Agents
Ketolides