New teixobactin analogues with a total lactam ring

Article

Scioli, G., Marinaccio, L., Bauer, M., Kamysz, W., Parmar, A., Newire, E., Singh, I., Stefanucci, A. and Mollica, A. 2023. New teixobactin analogues with a total lactam ring. ACS Medicinal Chemistry Letters. 14 (12), pp. 1603-1892. https://doi.org/10.1021/acsmedchemlett.3c00435
TypeArticle
TitleNew teixobactin analogues with a total lactam ring
AuthorsScioli, G., Marinaccio, L., Bauer, M., Kamysz, W., Parmar, A., Newire, E., Singh, I., Stefanucci, A. and Mollica, A.
Abstract

Teixobactin is a new antibiotic peptide with strong efficacy against several Gram-positive resistant bacteria, the structure of which is extremely difficult to obtain in the laboratory via multistep conventional synthesis. To face the increasing antibiotic resistant bacteria, it is fundamental to introduce new types of antibiotics with innovative mechanisms of action without resistance; thus, many scientists are studying and developing new methods to synthesize teixobactin analogues. In this work, seven Arg10-teixobactin analogues with a total lactam ring have been prepared via solid phase peptide synthesis. In order to obtain the total lactam ring, d-Thr8 was replaced by (2R,3S)-diamino-propionic acid. To verify their antimicrobial activity and efficacy, each analogue was tested with MIC against different resistant pathogens, showing an interesting activity for Nle11 containing compounds.

KeywordsTeixobactin; Cyclic peptide; Solid phase peptide synthesis; SPPS; Resin; Resistance; Bacteria
Sustainable Development Goals3 Good health and well-being
Middlesex University ThemeHealth & Wellbeing
PublisherAmerican Chemical Society (ACS)
JournalACS Medicinal Chemistry Letters
ISSN1948-5875
Publication dates
Online14 Nov 2023
Print14 Dec 2023
Publication process dates
Submitted25 Sep 2023
Accepted09 Nov 2023
Deposited16 Oct 2024
Output statusPublished
Publisher's version
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File Access Level
Open
Copyright Statement

Copyright © 2023 The Authors. Published by American Chemical Society. This publication is licensed under CC-BY 4.0 .

Digital Object Identifier (DOI)https://doi.org/10.1021/acsmedchemlett.3c00435
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