Solid-phase synthesis and antibacterial evaluations of N-demethylvancomycin derivatives

Nian-Huan Yao; Gang Liu; Wen-Yi He; Changqun Niu; James R Carlson; Kit S Lam

doi:10.1016/j.bmcl.2005.02.086

Solid-phase synthesis and antibacterial evaluations of N-demethylvancomycin derivatives

Bioorg Med Chem Lett. 2005 May 2;15(9):2325-9. doi: 10.1016/j.bmcl.2005.02.086.

Authors

Nian-Huan Yao¹, Gang Liu, Wen-Yi He, Changqun Niu, James R Carlson, Kit S Lam

Affiliation

¹ Chinese Academy of Medical Sciences & Peking Union Medical College, Institute of Materia Medica, 1 Xian Nong Tan Street, Beijing 100050, PR China.

PMID: 15837318
DOI: 10.1016/j.bmcl.2005.02.086

Abstract

Twenty-five N-demethylvancomycin derivatives were synthesized on solid-support and their structures were determined by LC-MS/MS. Biological evaluation of these compounds indicated that bulky hydrophobic substituent on vancosamine of N-demethylvancomycin can increase antibacterial activity against vancomycin-resistant Enterococcus faecalis.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Anti-Bacterial Agents / chemical synthesis*
Anti-Bacterial Agents / pharmacology
Enterococcus faecalis / drug effects
Indicators and Reagents
Microbial Sensitivity Tests
Molecular Structure
Staphylococcus aureus / drug effects
Structure-Activity Relationship
Vancomycin / analogs & derivatives
Vancomycin / chemical synthesis
Vancomycin / pharmacology

Substances

Anti-Bacterial Agents
Indicators and Reagents
Vancomycin
N-demethylvancomycin