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Yftah Tal‐Gan Monika Ivancic Gabriel Cornilescu Tian Yang Helen E. Blackwell 《Angewandte Chemie (Weinheim an der Bergstrasse, Germany)》2016,128(31):9059-9063
Blocking quorum sensing (QS) pathways has attracted considerable interest as an approach to suppress virulence in bacterial pathogens. Toward this goal, we recently developed analogues of a native autoinducing peptide (AIP‐III) signal that can inhibit AgrC‐type QS receptors and attenuate virulence phenotypes in Staphylococcus aureus. Application of these compounds is limited, however, as they contain hydrolytically unstable thioester linkages and have only low aqueous solubilities. Herein, we report amide‐linked AIP analogues with greatly enhanced hydrolytic stabilities and solubilities relative to our prior analogues, whilst maintaining strong potencies as AgrC receptor inhibitors in S. aureus. These compounds represent powerful tools for the study of QS. 相似文献
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Hamamelitannin Analogues that Modulate Quorum Sensing as Potentiators of Antibiotics against Staphylococcus aureus 下载免费PDF全文
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 《Angewandte Chemie (International ed. in English)》2016,55(22):6551-6555
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. 相似文献
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