期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 60, 期 21, 页码 8933-8944出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.7b01164
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资金
- NIH [5R21AI098689]
- University of Notre Dame
- Rempex Pharmaceuticals
- Medicines Company
Bromine induced lactamization of vinyl acetohydroxamates facilitated syntheses of monocyclic beta-lactams suitable for incorporation of a thiomethyl and extended functionality at the C(4) position. Elaboration of the resulting substituted N-hydroxy-2-azetidinones allowed incorporation of functionalized alpha-amino substituents appropriate for enhancement of antibiotic activity. Evaluation of antibacterial activity against a panel of Gram-positive and Gram-negative bacteria revealed structure-activity relationships (SAR) and identification of potent new monobactam antibiotics. The corresponding bis-catechol conjugate, 42, has excellent activity against Gram-negative bacteria including carbapenemase and carbacephalosporinase producing strains of Acinetobacter baumannii, which have been listed by the WHO as being of critical concern worldwide.
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