期刊
CHEMISTRY-A EUROPEAN JOURNAL
卷 26, 期 70, 页码 16875-16887出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.202003387
关键词
antibiotics; hybrid structures; natural products; nucleosides; structure-activity relationship
资金
- Deutsche Forschungsgemeinschaft (DFG) [DU 1095/5-1]
- Fonds der Chemischen Industrie (FCI)
- Projekt DEAL
To overcome bacterial resistances, the need for novel antimicrobial agents is urgent. The class of so-called nucleoside antibiotics furnishes promising candidates for the development of new antibiotics, as these compounds block a clinically unexploited bacterial target: the integral membrane protein MraY, a key enzyme in cell wall (peptidoglycan) biosynthesis. Nucleoside antibiotics exhibit remarkable structural diversity besides their uridine-derived core motifs. Some sub-classes also show specific selectivities towards different Gram-positive and Gram-negative bacteria, which are poorly understood so far. Herein, the synthesis of a novel hybrid structure is reported, derived from the 5'-defunctionalized uridine core moiety of muraymycins and the peptide chain of sansanmycin B, as a new scaffold for the development of antimicrobial agents. The reported muraymycin-sansanmycin hybrid scaffold showed nanomolar activity against the bacterial target enzyme MraY, but displayed no significant antibacterial activity against S. aureus, E. coli, and P. aeruginosa.
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