Valentina Straniero (Avtor), Victor Sebastián-Pérez (Avtor), Lorenzo Suigo (Avtor), William Margolin (Avtor), Andrea Casiraghi (Avtor), Martina Hrast (Avtor), Carlo Zanotto (Avtor), Irena Zdovc (Avtor), Antonia Radaelli (Avtor), Ermanno Valoti (Avtor)

Povzetek

Multidrug resistant Staphylococcus aureus is a severe threat, responsible for most of the nosocomial infections globally. This resistant strain is associated with a 64% increase in death compared to the antibiotic-susceptible strain. The prokaryotic protein FtsZ and the cell division cycle have been validated as potential targets to exploit in the general battle against antibiotic resistance. Despite the discovery and development of several anti-FtsZ compounds, no FtsZ inhibitors are currently used in therapy. This work further develops benzodioxane-benzamide FtsZ inhibitors. We seek to find more potent compounds using computational studies, with encouraging predicted drug-like profiles. We report the synthesis and the characterization of novel promising derivatives that exhibit very low MICs towards both methicillin-susceptible and -resistant S. aureus, as well as another Gram positive species, Bacillus subtilis, while possessing good predicted physical-chemical properties in terms of solubility, permeability, and chemical and physical stability. In addition, we demonstrate by fluorescence microscopy that Z ring formation and FtsZ localization are strongly perturbed by our derivatives, thus validating the target.

Ključne besede

Veterinarska medicina;

Podatki

Jezik: Angleški jezik
Leto izida:
Tipologija: 1.01 - Izvirni znanstveni članek
Organizacija: UL VF - Veterinarska fakulteta
UDK: 579:615.2:57.08
COBISS: 59812611 Povezava se bo odprla v novem oknu
ISSN: 2079-6382
Št. ogledov: 177
Št. prenosov: 40
Ocena: 0 (0 glasov)
Metapodatki: JSON JSON-RDF JSON-LD TURTLE N-TRIPLES XML RDFA MICRODATA DC-XML DC-RDF RDF

Ostali podatki

Sekundarni jezik: Slovenski jezik
Sekundarne ključne besede: Anti-Bacterial Agents;Pharmacology;Chemistry;Methicillin-Resistant Staphylococcus aureus;Bacillus subtilis;Drug resistance, microbial;Benzamides;Bacterial proteins;
Vrsta dela (COBISS): Članek v reviji
Strani: art. 442, str. 1-19
Letnik: ǂVol. ǂ10
Zvezek: ǂno. ǂ4
Čas izdaje: 2021
DOI: 10.3390/antibiotics10040442
ID: 14704359