New Antimicrobials Based on the Adarotene Scaffold with Activity against Multi-Drug Resistant Staphylococcus aureus and Vancomycin-Resistant Enterococcus

Antibiotics

Fabio Arena¹  Loana Musso²  Salvatore Princiotto²  Sabrina Dallavalle²  Stefania Mazzini²  Claudio Pisano³ 

[1] Centro di Ricerche Biomediche, Department of Clinical and Experimental Medicine, University of Foggia, Via Luigi Pinto, 71122 Foggia, Italy.;Department of Food, Environmental and Nutritional Sciences (DeFENS), Università degli Studi di Milano, Via Celoria 2, 20133 Milan, Italy;Preclinical Research&Biotech Development;

关键词: adarotene;    antimicrobials;    antimicrobial resistance;    Gram-positive;    bactericidal activity;   

DOI  :  10.3390/antibiotics10020126

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown