Cystobactamid 507 : Concise Synthesis, Mode of Action, and Optimization toward More Potent Antibiotics

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Elgaher, W.A.M.; Hamed, M.M.; Baumann, S.; Herrmann, J.; Siebenbürger, L.; et al.: Cystobactamid 507 : Concise Synthesis, Mode of Action, and Optimization toward More Potent Antibiotics. In: Chemistry - A European Journal 26 (2020), Nr. 32, S. 7219-7225. DOI:

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Sum total of downloads: 85

Lack of new antibiotics and increasing antimicrobial resistance are among the main concerns of healthcare communities nowadays, and these concerns necessitate the search for novel antibacterial agents. Recently, we discovered the cystobactamids—a novel natural class of antibiotics with broad-spectrum antibacterial activity. In this work, we describe 1) a concise total synthesis of cystobactamid 507, 2) the identification of the bioactive conformation using noncovalently bonded rigid analogues, and 3) the first structure–activity relationship (SAR) study for cystobactamid 507 leading to new analogues with high metabolic stability, superior topoisomerase IIA inhibition, antibacterial activity and, importantly, stability toward the resistant factor AlbD. Deeper insight into the mode of action revealed that the cystobactamids employ DNA minor-groove binding as part of the drug–target interaction without showing significant intercalation. By designing a new analogue of cystobactamid 919-2, we finally demonstrated that these findings could be further exploited to obtain more potent hexapeptides against Gram-negative bacteria. © 2020 The Authors. Published by Wiley-VCH Verlag GmbH & Co. KGaA.
License of this version: CC BY 4.0 Unported
Document Type: Article
Publishing status: publishedVersion
Issue Date: 2020
Appears in Collections:Naturwissenschaftliche Fakultät

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pos. country downloads
total perc.
1 image of flag of Germany Germany 39 45.88%
2 image of flag of No geo information available No geo information available 16 18.82%
3 image of flag of United States United States 14 16.47%
4 image of flag of China China 5 5.88%
5 image of flag of United Kingdom United Kingdom 2 2.35%
6 image of flag of France France 2 2.35%
7 image of flag of Netherlands Netherlands 1 1.18%
8 image of flag of Latvia Latvia 1 1.18%
9 image of flag of Indonesia Indonesia 1 1.18%
10 image of flag of Australia Australia 1 1.18%
    other countries 3 3.53%

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