Novel oxazolidinone antibacterials containing N-hydroxyacetamidine moiety are synthesized with the diversity at C-5 terminus. These compounds have been evaluated against a panel of clinically relevant gram-positive and gram-negative pathogens. Most of the analogs in this series displayed activity superior to Linezolid and in vivo efficacies of selected oxazolidinones are also disclosed herein.
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http://dx.doi.org/10.1016/j.bmcl.2006.01.109 | DOI Listing |
J Med Chem
January 2025
State Key Laboratory for Diagnosis and Treatment of Severe Zoonotic Infectious Diseases, Key Laboratory for Zoonosis Research of the Ministry of Education, Institute of Zoonosis, and College of Veterinary Medicine, Jilin University, Changchun 130062, China.
To date, the abuse of antibiotics and a gradual decline in novel antibiotic discovery enlarge the threat of drug-resistant bacterial infections, especially methicillin-resistant (MRSA). Herein, inspired by the unique structures and antibacterial activities of 2-quinolones, a class of novel 2-quinolones with substituted pyridines was synthesized. Notably, compound , the derivative with a methylpyridine fragment, showed potent antibacterial and antibiofilm activities, especially for MRSA strains (MIC = 0.
View Article and Find Full Text PDFPLoS One
January 2025
Dr. Rolf M. Schwiete Center for Limbal Stem Cell and Aniridia Research, Saarland University, Homburg/Saar, Germany.
Purpose: Rose Bengal Photodynamic Therapy (RB-PDT) offers dual therapeutic benefits by enhancing corneal stiffness and providing antibacterial activity, presenting significant potential for patients with keratoconus complicated by keratitis. Our purpose was to assess the effect of rose bengal photodynamic therapy (RB-PDT) on the expression of pro-inflammatory cytokines and chemokines, as well as on extracellular matrix (ECM)-related molecules, in lipopolysaccharide (LPS)-induced inflammation of keratoconus human corneal fibroblasts (KC-HCFs). Additionally, the involvement of the mitogen-activated protein kinase (MAPK) and nuclear factor kappa B (NF-κB) signaling pathways which are downstream of the Toll-like receptor 4 (TLR4) pathway were examined.
View Article and Find Full Text PDFPLoS One
January 2025
Department of Prosthodontics, Faculty of Dentistry, University of the Western Cape, Cape Town, South Africa.
Introduction: The global prevalence of antimicrobial resistance transcends geographical and economic boundaries, affecting populations worldwide. Excessive and incorrect use of antibiotics encourages antimicrobial resistance which leads to complex treatment strategies for infectious diseases and possible failure of treatment. The incorrect and unnecessary prescribing of antibiotics places a burden on healthcare costs and thus, antimicrobial resistance is evident globally as a major public health concern.
View Article and Find Full Text PDFMicrobiol Spectr
January 2025
School of Pharmacy, Lanzhou University, Lanzhou, China.
Colorectal cancer (CRC) is a common cancer accompanied by microbiome dysbiosis. Exploration of probiotics against oncogenic microorganisms is promising for CRC treatment. Here, differential microorganisms between CRC and healthy control were analyzed.
View Article and Find Full Text PDFJ Med Microbiol
January 2025
Laboratory of Molecular Microbiology (Micromol), Institute of Biomedical Sciences, Universidade Federal de Uberlndia, Uberlndia, Minas Gerais, Brazil.
In critically ill patients, the occurrence of multidrug-resistant infection is a significant concern, given its ability to acquire multidrug-resistant, form biofilms and secrete toxic effectors. In Brazil, limited data are available regarding the prevalence of dissemination, and the impact of the type III secretion system (T3SS) on toxin production and biofilm formation in clinical isolates of . This study investigates the dissemination of virulent harbouring the and genes, the presence of T3SS genes and their biofilm-forming capability.
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