Design, synthesis and biological evaluation of novel hamamelitannin analogues as potentiators for vancomycin in the treatment of biofilm related Staphylococcus aureus infections.

Abstract

Staphylococcus aureus is a frequent cause of biofilm-related infections. Bacterial cells within a biofilm are protected from attack by the immune system and conventional antibiotics often fail to penetrate the biofilm matrix. The discovery of hamamelitannin as a potentiator for antibiotics, recently led to the design of a more drug-like lead. In the present study, we want to gain further insight into the structure-activity relationship (S.A.R.) of the 5-position of the molecule, by preparing a library of 21 hamamelitannin analogues.

• Authors: Arno Vermote, Gilles Brackman, Martijn D P Risseeuw, Tom Coenye, Serge Van Calenbergh
• Journal: Bioorganic & medicinal chemistry (Bioorg Med Chem) Vol. 24 Issue 19 Pg. 4563-4575 (10 01 2016) ISSN: 1464-3391 [Electronic] England
• PMID: 27507109 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2016 Elsevier Ltd. All rights reserved.

Chemical References

• Anti-Bacterial Agents
• Hexoses
• Gallic Acid
• Vancomycin
• hamamelitannin

Topics

• Anti-Bacterial Agents (chemistry, pharmacology)
• Biofilms (drug effects)
• Drug Design
• Gallic Acid (analogs & derivatives, chemistry, pharmacology)
• Hexoses (chemistry, pharmacology)
• Humans
• Microbial Sensitivity Tests
• Quorum Sensing (drug effects)
• Staphylococcal Infections (drug therapy)
• Staphylococcus aureus (drug effects, physiology)
• Structure-Activity Relationship
• Vancomycin (pharmacology)