期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 63, 期 15, 页码 8359-8368出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.0c00584
关键词
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资金
- European Research Council (ERC) [757913]
- Helmholtz-Association's Initiative and Networking Fund
- Austrian Science Fund (FWF) [P31843]
- Alexander von Humboldt Foundation
- Austrian Science Fund (FWF) [P31843] Funding Source: Austrian Science Fund (FWF)
In light of the global antimicrobial-resistance crisis, there is an urgent need for novel bacterial targets and antibiotics with novel modes of action. It has been shown that Pseudomonas aeruginosa elastase (LasB) and Clostridium histolyticum (Hathewaya histolytica) collagenase (CoIH) play a significant role in the infection process and thereby represent promising antivirulence targets. Here, we report novel N-aryl-3-mercaptosuccinimide inhibitors that target both LasB and CoIH, displaying potent activities in vitro and high selectivity for the bacterial over human metalloproteases. Additionally, the inhibitors demonstrate no signs of cytotoxicity against selected human cell lines and in a zebrafish embryo toxicity model. Furthermore, the most active CoIH inhibitor shows a significant reduction of collagen degradation in an ex vivo pig-skin model.
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