Design, synthesis and biological evaluation of novel hamamelitannin analogues as potentiators for vancomycin in the treatment of biofilm related Staphylococcus aureus infections. Issue 19 (1st October 2016)

• Record Type: Journal Article
• Authors: Vermote, Arno; Brackman, Gilles; Risseeuw, Martijn D.P.; Coenye, Tom; Van Calenbergh, Serge
• Is Part Of: Bioorganic & medicinal chemistry. Volume 24:Issue 19(2016)
• Page Start: 4563
• Page End: 4575
• Publication Date: 2016-10-01
• Subjects: Hamamelitannin analogues -- Antibiotic potentiators -- Quorum sensing -- Staphylococcus aureus -- Biofilms; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2016.07.058
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: 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.