The global increase in infections by multi-drug resistant (MDR) pathogens is severely impacting our ability to successfully treat common infections. Herein, we report the antibacterial activity against S. aureus and E. faecalis (including some MDR strains) of a panel of adarotene-related synthetic retinoids. In many cases, these compounds showed, together with favorable MICs, a detectable bactericidal effect. We found that the pattern of substitution on adarotene could be modulated to obtain selectivity for antibacterial over the known anticancer activity of these compounds. NMR experiments allowed us to define the interaction between adarotene and a model of microorganism membrane. Biological assessment confirmed that the scaffold of adarotene is promising for further developments of non-toxic antimicrobials active on MDR strains.

New antimicrobials based on the adarotene scaffold with activity against multi-drug resistant staphylococcus aureus and vancomycin-resistant enterococcus / S. Princiotto, S. Mazzini, L. Musso, F. Arena, S. Dallavalle, C. Pisano. - In: ANTIBIOTICS. - ISSN 2079-6382. - 10:2(2021 Feb), pp. 126.1-126.13.

New antimicrobials based on the adarotene scaffold with activity against multi-drug resistant staphylococcus aureus and vancomycin-resistant enterococcus

Princiotto S.;Mazzini S.;Musso L.;Dallavalle S.;
2021-02

Abstract

The global increase in infections by multi-drug resistant (MDR) pathogens is severely impacting our ability to successfully treat common infections. Herein, we report the antibacterial activity against S. aureus and E. faecalis (including some MDR strains) of a panel of adarotene-related synthetic retinoids. In many cases, these compounds showed, together with favorable MICs, a detectable bactericidal effect. We found that the pattern of substitution on adarotene could be modulated to obtain selectivity for antibacterial over the known anticancer activity of these compounds. NMR experiments allowed us to define the interaction between adarotene and a model of microorganism membrane. Biological assessment confirmed that the scaffold of adarotene is promising for further developments of non-toxic antimicrobials active on MDR strains.
Adarotene; Antimicrobial resistance; Antimicrobials; Bactericidal activity; Gram-positive
Settore CHIM/06 - Chimica Organica
28-gen-2021
ANTIBIOTICS
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2434/822099
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