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

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

来源：ACS Medicinal Chemistry Letters, 2017, 8(1): 38-42.

DOI：10.1021/acsmedchemlett.6b00315

• Antibiotic potentiators
• Staphylococcus aureus
• hamamelitannin analogues
• quorum sensing
• biofilms

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 mu M.

• 出版日期2017-1