期刊
CHEMMEDCHEM
卷 11, 期 17, 页码 1899-1903出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201600231
关键词
albicidin; antibacterials; antibiotics; gyrase; para-aminobenzoic acid; peptides
资金
- Fonds der Chemischen Industrie
- City of Berlin (Elsa-Neumann-Fellowship)
- AlbiPharm-BMBF VIP+ [03VP00030]
The peptide antibiotic albicidin, which is synthesized by the plant pathogenic bacterium, Xanthomonas albilineans, represents the most prominent member of a new class of antibacterial gyrase inhibitors. It shows remarkable antibacterial activities against Gram-positive and Gram-negative microorganisms. Its unique structure potentially represents a new lead structure for the development of an antibacterial drug. Here we report the synthesis of 14 albicidin derivatives with structural variations at the N-terminus, primarily investigating the effects of variation of cinnamoyl, phenylpropanoyl, and benzoyl residues. Gyrase inhibition in vitro and determination of minimal inhibitory concentrations were assessed in parallel. Activities in a nanomolar range and the importance of N-acylation were demonstrated.
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