Journal
ORGANIC LETTERS
Volume 23, Issue 18, Pages 7023-7027Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.1c02312
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Funding
- Deutsche Forschungsgemeinschaft (DFG) [SU 239/11-1, PE 2600/1-1, RTG 2473]
- Alexander-von-Humboldt-Foundation
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A study synthesized and evaluated six analogues of albicidin with isosteric replacement of the key amide link, achieving protease stability while maintaining antibacterial activity. Three analogues showed up to eight times higher antibacterial activity compared to natural albicidin.
Albicidin is a potent antibacterial oligoaromatic peptide that is susceptible to the protease AlbD, a resistance factor. This potentially restricts the use of albicidin as a drug. To overcome this obstacle, we synthesized and evaluated six analogues with isosteric replacement of the key amide link. Protease stability was established while maintaining the antibacterial activity, including three analogues with up to eight times higher activity compared with the natural albicidin.
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