Issue 4, 2017

Synthesis and structure–activity relationship studies of teixobactin analogues

Abstract

A new series of teixobactin analogues were synthesized via an oxidative cyclative cleavage approach using aryl hydrazide resin as the solid support. Structure–activity relationship studies revealed that the guanidine or amine group at position 10, the hydroxyl group of Ser7 residue and the NH proton of the N-terminal Phe1 residue are critical to the antibacterial activities, while side chain size and functional group changes are tolerated at position 4. These findings will facilitate the development of new teixobactin analogues with enhanced pharmacological properties.

Graphical abstract: Synthesis and structure–activity relationship studies of teixobactin analogues

Supplementary files

Article information

Article type
Paper
Submitted
09 nov 2016
Accepted
01 dec 2016
First published
12 jan 2017
This article is Open Access
Creative Commons BY-NC license

RSC Adv., 2017,7, 1923-1926

Synthesis and structure–activity relationship studies of teixobactin analogues

C. Wu, Z. Pan, G. Yao, W. Wang, L. Fang and W. Su, RSC Adv., 2017, 7, 1923 DOI: 10.1039/C6RA26567G

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