Hamamelitannin Analogues that Modulate Quorum Sensing as Potentiators of Antibiotics against Staphylococcus aureus |
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| Authors: | Arno Vermote Dr. Gilles Brackman Dr. Martijn D. P. Risseeuw Bieke Vanhoutte Prof. Dr. Paul Cos Prof. Dr. Kristof Van Hecke Dr. Koen Breyne Prof. Dr. Evelyne Meyer Prof. Dr. Tom Coenye Prof. Dr. Serge Van Calenbergh |
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| Affiliation: | 1. Laboratory for Medicinal Chemistry, Ghent University, Ghent, Belgium;2. Laboratory for Pharmaceutical Microbiology, Ghent University, Ghent, Belgium;3. Laboratory for Microbiology, Parasitology and Hygiene, University of Antwerp, Wilrijk, Belgium;4. XStruct, Department of Inorganic and Physical Chemistry, Ghent University, Ghent, Belgium;5. Laboratory of Biochemistry, Ghent Univeristy, Merelbeke, Belgium |
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| Abstract: | The modulation of bacterial communication to potentiate the effect of existing antimicrobial drugs is a promising alternative to the development of novel antibiotics. In the present study, we synthesized 58 analogues of hamamelitannin (HAM), a quorum sensing inhibitor and antimicrobial potentiator. These efforts resulted in the identification of an analogue that increases the susceptibility of Staphylococcus aureus towards antibiotics in vitro, in Caenorhabditis elegans, and in a mouse mammary gland infection model, without showing cytotoxicity. |
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| Keywords: | antibiotics biofilms MRSA potentiators quorum sensing |
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