期刊
CHEMMEDCHEM
卷 6, 期 5, 页码 840-847出版社
WILEY-BLACKWELL
DOI: 10.1002/cmdc.201000539
关键词
antibacterial activity; azole; gramicidin S; hemolytic activity; peptides
资金
- Xunta de Galicia
- Spanish Ministry of Science and Innovation [BFU2008-01588]
- STW [07109]
The influence of replacing the D-phenylalanine residue with substituted and unsubstituted azoles on the structure and biological activity of the antibiotic gramicidin S was investigated against a representative panel of Gram-positive and Gram-negative bacteria strains. Substituted triazole derivatives, obtained using a convergent synthetic strategy, are as active as gramicidin S, provided that any substituent on the triazole moiety is not too large. The unsubstituted triazole derivative was biologically less active than the parent natural product, gramicidin S. In general for the triazole series, the hemolytic activity could be correlated with the antibacterial activity, that is, the higher the antibacterial activity, the higher the toxicity towards blood cells. Interestingly, its imidazole counterpart showed high antibacterial activity, combined with significantly diminished hemolytic activity.
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