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Thirty-two new naphthylthiazole derivatives were synthesized with the aim of exploring their antimicrobial effect on multidrug-resistant Gram-positive bacteria. Compounds 25 and 32, with ethylenediamine and methylguanidine side chains, represent the most promising derivatives, as their antibacterial spectrum includes activity against multidrug-resistant staphylococcal and enterococcal strains. Moreover, the new derivatives are highly advantageous over the existing frontline therapeutics for the treatment of multidrug-resistant Gram-positive bacteria. In this vein, compound 25 possesses three attributes: no bacterial resistance was developed against it even after 15 passages, it was very efficient in targeting intracellular pathogens, and it exhibited a concentration-dependent ability to disrupt the preformed bacterial biofilm.
This article was published in the following journal.
Name: ACS infectious diseases
Domestic animals can serve as reservoirs for drug resistant S. aureus and may lead to the emergence of multidrug resistant human S. aureus.
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A strain of Staphylococcus aureus that is non-susceptible to the action of METHICILLIN. The mechanism of resistance usually involves modification of normal or the presence of acquired PENICILLIN BINDING PROTEINS.
A species of STAPHYLOCOCCUS similar to STAPHYLOCOCCUS HAEMOLYTICUS, but containing different esterases. The subspecies Staphylococcus hominis novobiosepticus is highly virulent and novobiocin resistant.
A 25-kDa peptidase produced by Staphylococcus simulans which cleaves a glycine-glcyine bond unique to an inter-peptide cross-bridge of the STAPHYLOCOCCUS AUREUS cell wall. EC 22.214.171.124.
Pneumonia caused by infections with bacteria of the genus STAPHYLOCOCCUS, usually with STAPHYLOCOCCUS AUREUS.
A COAGULASE-negative species of STAPHYLOCOCCUS found on the skin and MUCOUS MEMBRANE of warm-blooded animals. Similar to STAPHYLOCOCCUS EPIDERMIDIS and STAPHYLOCOCCUS HAEMOLYTICUS, it is a nosocomial pathogen in NICU settings. Subspecies include generally antibiotic susceptible and BIOFILM negative capitis and antibiotic resistant and biofilm positive urealyticus isolates.