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Synlett 2015; 26(09): 1175-1178
DOI: 10.1055/s-0034-1380509
DOI: 10.1055/s-0034-1380509
letter
Synthesis and Biological Evaluation of Cystobactamid 507: A Bacterial Topoisomerase Inhibitor from Cystobacter sp.
Further Information
Publication History
Received: 26 January 2015
Accepted after revision: 05 March 2015
Publication Date:
01 April 2015 (online)
![](https://www.thieme-connect.de/media/synlett/201509/lookinside/thumbnails/st-2015-b0058-l_10-1055_s-0034-1380509-1.jpg)
Abstract
The first total synthesis of cystobactamid 507, a member of a class of new natural products with strong inhibitory activity towards bacterial topoisomerases, is reported. Synthetic key challenges are the central tetrasubstitued arene and the low chemical reactivity of anilines and ortho-phenolic and isopropoxy-substituted benzoic acids. Biological evaluations demonstrate that cystobactamid 507 inhibits several Gram-positive pathogens but at significantly lower concentrations than described for the larger members of this natural product family.
Supporting Information
- Supporting information for this article is available online at http://dx.doi.org/10.1055/s-0034-1380509. Included are experimental procedures, spectral data and copies of 1H and 13C NMR spectra of all new compounds and intermediates.
- Supporting Information
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