Abstract
The in vitro activities of five quinazolinone antibacterials, compounds Q1 to Q5, were tested against 210 strains of methicillin-resistant Staphylococcus aureus (MRSA). The MIC50/MIC90 values (in μg/ml) were as follows: Q1, 0.5/2; Q2, 1/4; Q3, 2/4; Q4, 0.06/0.25; and Q5, 0.125/0.5. Several strains with high MIC values (from 8 to >32 μg/ml) for some of these compounds exhibited amino acid changes in the penicillin-binding proteins, which are targeted by these antibacterials.
Highlights
Nosocomial and community-acquired methicillin-resistant Staphylococcus aureus (MRSA) infections remain major clinical problems
We have described the discovery of the quinazolinones as cell wall-active antibacterials with anti-S. aureus activity, including MRSA strains [7]
We investigated the antibacterial activity profile of five quinazolinones of our design, compounds Q1 to Q5 (Fig. 1), against a collection of 210 MRSA strains (108 strains from the United States and 102 from Spain)
Summary
Sara Ceballos,a Choon Kim,b Yuanyuan Qian,b Shahriar Mobashery,b Mayland Chang,b Carmen Torresa aArea of Biochemistry and Molecular Biology, University of La Rioja, Logroño, Spain bDepartment of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, Indiana, USA
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