Synthesis and SAR studies of novel benzodiazepinedione-based inhibitors of Clostridium difficile (C. difficile) toxin B (TcdB).

Bioorganic & Medicinal Chemistry Letters(2018)

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摘要
•Highly potent C. diff. toxin B (TcdB) inhibitors identified.•Improved plasma stability enabled compound progression into in vivo models of CDI.•Compound 11d efficacious in hamster survival model of CDI upon oral dosing.
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关键词
Clostridium difficile,Toxin,TcdB,Inhibitor,Benzodiazepinedione
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