Issue 4, 2016

Concurrent modifications of the C-terminus and side ring of thiostrepton and their synergistic effects with respect to improving antibacterial activities

Abstract

The double-mutant strain Streptomyces laurentii ΔtsrB/T was designed and constructed based on a recent understanding regarding the structure–activity relationship of thiostrepton (TSR) against prokaryotic pathogens. Five new C-terminally methylated TSR (CmTSR) derivatives that varied in the side-ring structure were obtained via the chemical feeding of quinaldic acid (QA) analogs. These derivatives provide new insights into the tolerance of QA incorporation in TSR biosynthesis. Certain members of the tested TSR derivatives, meanwhile, exhibited much better antibacterial activities than all currently known thiopeptide antibiotics.

Graphical abstract: Concurrent modifications of the C-terminus and side ring of thiostrepton and their synergistic effects with respect to improving antibacterial activities

Supplementary files

Article information

Article type
Research Article
Submitted
22 Kax 2015
Accepted
08 Nah 2016
First published
09 Nah 2016

Org. Chem. Front., 2016,3, 496-500

Concurrent modifications of the C-terminus and side ring of thiostrepton and their synergistic effects with respect to improving antibacterial activities

S. Wang, Q. Zheng, J. Wang, D. Chen, Y. Yu and W. Liu, Org. Chem. Front., 2016, 3, 496 DOI: 10.1039/C5QO00433K

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