New Teixobactin Analogues with a Total Lactam Ring

Scioli, Giuseppe, Marinaccio, Lorenza, Bauer, Marta, Kamysz, Wojciech, Parmar, Anish, Newire, Enas, Singh, Ishwar ORCID: 0000-0001-7822-1063, Stefanucci, Azzurra and Mollica, Adriano (2023) New Teixobactin Analogues with a Total Lactam Ring. ACS Medicinal Chemistry Letters, 14 (12). pp. 1827-1832.

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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 (2<i>R</i>,3<i>S</i>)-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.

Item Type:	Article
Uncontrolled Keywords:	Infectious Diseases, Emerging Infectious Diseases, Antimicrobial Resistance, 5.1 Pharmaceuticals, 5 Development of treatments and therapeutic interventions, Infection
Divisions:	Faculty of Health and Life Sciences Faculty of Health and Life Sciences > Institute of Systems, Molecular and Integrative Biology
Depositing User:	Symplectic Admin
Date Deposited:	20 Nov 2023 08:50
Last Modified:	15 Mar 2024 17:09
DOI:	10.1021/acsmedchemlett.3c00435
Related URLs:	Author Publisher
URI:	https://livrepository.liverpool.ac.uk/id/eprint/3176886