Novel Potentiators for Vancomycin in the Treatment of Biofilm-Related MRSA Infections via a Mix and Match Approach

Arno Vermote; Gilles Brackman; Martijn D P Risseeuw; Davie Cappoen; Paul Cos; Tom Coenye; Serge Van Calenbergh

doi:10.1021/acsmedchemlett.6b00315

Novel Potentiators for Vancomycin in the Treatment of Biofilm-Related MRSA Infections via a Mix and Match Approach

ACS Med Chem Lett. 2016 Nov 9;8(1):38-42. doi: 10.1021/acsmedchemlett.6b00315. eCollection 2017 Jan 12.

Authors

Arno Vermote¹, Gilles Brackman², Martijn D P Risseeuw¹, Davie Cappoen³, Paul Cos³, Tom Coenye², Serge Van Calenbergh¹

Affiliations

¹ Laboratory for Medicinal Chemistry, Ghent University , Ottergemsesteenweg 460, B-9000 Ghent, Belgium.
² Laboratory for Pharmaceutical Microbiology, Ghent University , Ottergemsesteenweg 460, B-9000 Ghent, Belgium.
³ Laboratory for Microbiology, Parasitology and Hygiene, University of Antwerp , Universiteitsplein 1 (S7), B-2610 Wilrijk, Belgium.

Abstract

A library of 52 hamamelitannin analogues was synthesized and investigated for its ability to potentiate the effect of vancomycin toward Staphylococcus aureus biofilms. Several compounds were found to effectively increase the susceptibility of staphylococcal biofilms toward this glycopeptide. The most active analogue identified in this study showed an EC₅₀ value of 0.26 μM.

Keywords: Antibiotic potentiators; Staphylococcus aureus; biofilms; hamamelitannin analogues; quorum sensing.