Synthesis and biological properties of macrolactam analogs of the natural product macrolide (-)-A26771B

Sophie Canova; Renaud Lépine; Amber Thys; Anne Baron; Didier Roche

doi:10.1016/j.bmcl.2011.06.073

Synthesis and biological properties of macrolactam analogs of the natural product macrolide (-)-A26771B

Bioorg Med Chem Lett. 2011 Aug 15;21(16):4768-72. doi: 10.1016/j.bmcl.2011.06.073. Epub 2011 Jun 23.

Authors

Sophie Canova¹, Renaud Lépine, Amber Thys, Anne Baron, Didier Roche

Affiliation

¹ Edelris, 115 Avenue Lacassagne, 69003 Lyon, France.

PMID: 21767951
DOI: 10.1016/j.bmcl.2011.06.073

Abstract

Promising synthetic derivatives of macrolactone natural product (-)-A26771B have been designed and synthesized both from semisynthesis and total synthesis. Further optimization led to the first synthesis of macrolactam analogs of (-)-A26771B with improved antibacterial activity and metabolic stability.

MeSH terms

Anti-Bacterial Agents / chemical synthesis
Anti-Bacterial Agents / metabolism
Anti-Bacterial Agents / pharmacology*
Bacteria / drug effects*
Biological Factors / chemical synthesis
Biological Factors / metabolism
Biological Factors / pharmacology*
Dose-Response Relationship, Drug
Drug Design
Lactones / chemical synthesis
Lactones / metabolism
Lactones / pharmacology
Microbial Sensitivity Tests
Molecular Structure
Stereoisomerism
Structure-Activity Relationship

Substances

Anti-Bacterial Agents
Biological Factors
Lactones
A26771B