Discovery of mercaptopropanamide-substituted aryl tetrazoles as new broad-spectrum metallo-β-lactamase inhibitors
نویسندگان
چکیده
منابع مشابه
Diaryl-substituted azolylthioacetamides: Inhibitor discovery of New Delhi metallo-β-lactamase-1 (NDM-1).
The emergence and spread of antibiotic-resistant pathogens is a global public health problem. Metallo-β-lactamases (MβLs) such as New Delhi MβL-1 (NDM-1) are principle contributors to the emergence of resistance because of their ability to hydrolyze almost all known β-lactam antibiotics including penicillins, cephalosporins, and carbapenems. A clinical inhibitor of MBLs has not yet been found. ...
متن کاملNew Delhi Metallo-β-Lactamase, Ontario, Canada
To the Editor: The New Delhi metallo-β-lactamase (NDM-1) was fi rst characterized in 2009 from Kleb-siella pneumoniae and Escherichia coli isolated from a patient in Sweden who had received medical care in New Delhi, India (1). Further studies have shown broad dissemination of this β-lactamase gene (bla NDM-1) in India, Pakistan, Bangladesh, and the United Kingdom (2). Additional isolates have ...
متن کاملOligopeptides as full-length New Delhi metallo-β-lactamase-1 (NDM-1) inhibitors
'Superbug' bacteria producing NDM-1 enzyme causing wide public concern were first detected in a patient who visited India in 2008. It's an effective approach to combining β-lactam antibiotics with NDM-1 inhibitor for treating NDM-1 producing strain infection. In our research, we designed ten oligopeptides, tested IC50 values against NDM-1 enzyme, determined the MIC values of synergistic antibac...
متن کاملOverview Metallo-β-lactamase inhibitors: Promise for the future?
Carbapenem resistance continues to erode the effectiveness of antibiotics such as imipenem and meropenem in the clinic. Resistance mechanisms can include interplay between porin loss (membrane permeability), mutation of penicillin binding proteins necessary for cell division, and expression of class A, B and D β-lactamases. Bacterial resistance to β-lactams such as penicillin or amoxicillin has...
متن کاملInhibitor Discovery of Full-Length New Delhi Metallo-β-Lactamase-1 (NDM-1)
New Delhi metallo-β-lactmase-1 (NDM-1) has recently attracted extensive attention for its biological activities to catalyze the hydrolysis of almost all of β-lactam antibiotics. To study the catalytic property of NDM-1, the steady-kinetic parameters of NDM-1 toward several kinds of β-lactam antibiotics have been detected. It could effectively hydrolyze most β-lactams (k cat/K m ratios between 0...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: RSC Advances
سال: 2020
ISSN: 2046-2069
DOI: 10.1039/d0ra06405j