6-beta-bromopenicillanic acid, a potent beta-lactamase inhibitor.
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چکیده
منابع مشابه
Synthesis of deuterium- and tritium-labeled 6 beta-bromopenicillanic acid.
The synthesis of 6 beta-bromopenicillanic acid labeled with deuterium and tritium in the beta-methyl group is described. The S-sulfoxide of benzyl- or p-methoxybenzyl 6 alpha-bromopenicillanate is refluxed in benzene containing an excess of tert-BuOD, D2O or HTO. After deoxygenation and deprotection of the ester, the labeled 6 alpha-bromopenicillanic acid is epimerized (N,O-bis(trimethylsilyl)a...
متن کاملActivity of beta-lactam beta-lactamase inhibitor combinations against extended spectrum Beta-lactamase producing Enterobacteriaceae in urinary isolates.
OBJECTIVE To determine the susceptibility pattern of beta-lactam beta-lactamase inhibitor combinations against extended-spectrum beta-lactamase (ESBL) producing Enterobacteriaceae in urinary isolates. STUDY DESIGN Observational study. PLACE AND DURATION OF STUDY Ziauddin University Hospital, Karachi, from February to October 2008. METHODOLOGY A total of 190 consecutive non-duplicate isola...
متن کاملThermodynamic cycle analysis and inhibitor design against beta-lactamase.
Beta-lactamases are the most widespread resistance mechanism to beta-lactam antibiotics, such as the penicillins and cephalosporins. Transition-state analogues that bind to the enzymes with nanomolar affinities have been introduced in an effort to reverse the resistance conferred by these enzymes. To understand the origins of this affinity, and to guide design of future inhibitors, double-mutan...
متن کاملComparative in vitro activity of beta-lactam/beta-lactamase inhibitor combinations against gram negative bacteria.
BACKGROUND & OBJECTIVE Currently, the use of beta-lactamase inhibitors in combination with beta-lactam antibiotics represents an effective measure to combat a specific resistance mechanism of beta-lactamase producing organisms. Knowledge about the susceptibility profile of bacteria to different combination agents available is essential to guide appropriate treatment of severe infections in hosp...
متن کاملBeta-Lactamase Inhibitor That Extends the Antibacterial Spectrum of Beta-Lactams: Initial Bacteriological Characterization
CP-45,899 {3,3-dimethyl-7-oxo-4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid, 4,4-dioxide, [2S-(2a,5a)]} is an irreversible inhibitor of several bacterial penicillinases and cephalosporinases. In the presence oflow concentrations of CP45,899, ampicillin and other f,-lactams readily inhibit the growth of a variety of resistant bacteria that contain ,-lactamases. CP-45,899 used alone display...
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ژورنال
عنوان ژورنال: Proceedings of the National Academy of Sciences
سال: 1978
ISSN: 0027-8424,1091-6490
DOI: 10.1073/pnas.75.9.4145