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marzo 2021

Polymyxins for the treatment of lower respiratory tract infections; lessons learned from the integration of clinical pharmacokinetic studies and clinical outcomes

The global rise in nosocomial pneumonia caused by multidrug-resistant (MDR) Gram-negative pathogens and increasingly limited antibiotic treatment options are growing threats to modern medicine. As a result, older antibiotics like polymyxins are being used as drugs of last resort for MDR nosocomial pneumonia. Polymyxins are bactericidal against most aerobic Gram-negative bacilli, but the sub-therapeutic concentrations achieved at infection sites following high-dose intravenous administration make…

In silico guided design of non-covalent inhibitors of DprE1: synthesis and biological evaluation

DprE1 is a potential target of resistant tuberculosis (TB), especially multidrug-resistant (MDR) and extensively drug-resistant (XDR) TB. 2-benzoxazolinone is a closely related bioisostere of some scaffolds such as benzoxazoles, benzimidazole, benzothiazolinone, and benzothiazoles that have been previously explored against DprE1. Thus, a ligand-based quantitative pharmacophore model (AHRR.8) of DprE1 was developed and this pharmacophore model was utilized in activity profiling of some…

Antibacterial, anti-inflammatory and antioxidant activities of Mahanintangtong and its constituent herbs, a formula used in Thai traditional medicine for treating pharyngitis

CONCLUSION: The ethanol extracts from carbonized T. grandis and Mahanintangtong showed good antimicrobial activity, especially against S. pyogenes, and good anti-inflammatory activity. These findings are relevant to the pathogenesis of pharyngitis and justify additional studies to see if Mahanintangtong could have clinical utility.

The global dissemination of hospital clones of Enterococcus faecium

CONCLUSIONS: The ability of A1 E. faecium to continually present new combinations of genes for potential selection suggests that controlling this pathogen will remain challenging but establishing a framework for understanding genomic evolution is likely to aid in tracking the threats posed by newly emerging lineages.