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- 2021 (1) (entfernen)
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- Englisch (1)
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- Rh(II) catalysis (1)
- diazo compounds (1)
- metallo β lactamases (1)
- multiresistant bacteria (1)
- thiol inhibitors (1)
Institut
Diversity-oriented synthesis (DOS) is a rich source for novel lead structures in Medicinal Chemistry. In this study, we present a DOS-compatible method for synthesis of compounds bearing a free thiol moiety. The procedure relies on Rh(II)-catalyzed coupling of dithiols to diazo building blocks. The synthetized library was probed against metallo-β-lactamases (MBLs) NDM-1 and VIM-1. Biochemical and biological evaluation led to identification of novel potent MBL inhibitors with antibiotic adjuvant activity.