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Title

Discovery of antibiotic (E)-3-(3-carboxyphenyl)-2-(4-cyanostyryl)quinazolin-4(3 H)-one

AuthorsBouley, R.; Kumarasiri, M.; Peng, Z.; Otero, L. H.; Song, W.; Suckow, M.A.; Schroeder, V.A.; Wolter, W.R.; Lastochkin, E.; Antunes, N.T.; Pi, H.; Vakulenko, S.; Hermoso, Juan A. CSIC ORCID; Chang, M.; Mobashery, S.
Issue Date2015
PublisherAmerican Chemical Society
CitationJournal of the American Chemical Society 137: 1738- 1741 (2015)
Abstract© 2015 American Chemical Society. In the face of the clinical challenge posed by resistant bacteria, the present needs for novel classes of antibiotics are genuine. In silico docking and screening, followed by chemical synthesis of a library of quinazolinones, led to the discovery of (E)-3-(3-carboxyphenyl)-2-(4-cyanostyryl)quinazolin-4(3H)-one (compound 2) as an antibiotic effective in vivo against methicillin-resistant Staphylococcus aureus (MRSA). This antibiotic impairs cell-wall biosynthesis as documented by functional assays, showing binding of 2 to penicillin-binding protein (PBP) 2a. We document that the antibiotic also inhibits PBP1 of S. aureus, indicating a broad targeting of structurally similar PBPs by this antibiotic. This class of antibiotics holds promise in fighting MRSA infections.
URIhttp://hdl.handle.net/10261/130611
DOI10.1021/jacs.5b00056
Identifiersdoi: 10.1021/jacs.5b00056
issn: 1520-5126
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