title: 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: Laboratory for Medicinal Chemistry, Ghent University, Ottergemsesteenweg 460, B-9000 Ghent, Belgium.
authors: Arno
authors: A
authors: Vermote
authors: Laboratory for Pharmaceutical Microbiology, Ghent University, Ottergemsesteenweg 460, B-9000 Ghent, Belgium.
authors: Gilles
authors: G
authors: Brackman
authors: Laboratory for Medicinal Chemistry, Ghent University, Ottergemsesteenweg 460, B-9000 Ghent, Belgium.
authors: Martijn D P
authors: MDP
authors: Risseeuw
authors: Laboratory for Pharmaceutical Microbiology, Ghent University, Ottergemsesteenweg 460, B-9000 Ghent, Belgium.
authors: Tom
authors: T
authors: Coenye
authors: Laboratory for Medicinal Chemistry, Ghent University, Ottergemsesteenweg 460, B-9000 Ghent, Belgium. Electronic address: serge.vancalenbergh@ugent.be.
authors: Serge
authors: S
authors: Van Calenbergh
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology*; D018441:Biofilms / Q000187:drug effects*; D015195:Drug Design; D005707:Gallic Acid / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D006601:Hexoses / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D008826:Microbial Sensitivity Tests; D053038:Quorum Sensing / Q000187:drug effects; D013203:Staphylococcal Infections / Q000188:drug therapy; D013211:Staphylococcus aureus / Q000187:drug effects* / Q000502:physiology; D013329:Structure-Activity Relationship; D014640:Vancomycin / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D006601:Hexoses; D005707:Gallic Acid; D014640:Vancomycin; C093412:hamamelitannin
keywords: Antibiotic potentiators; Biofilms; Hamamelitannin analogues; Quorum sensing; Staphylococcus aureus