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dc.contributor.author
Bouley, Renee
dc.contributor.author
Kumarasiri, Malika
dc.contributor.author
Peng, Zhihong
dc.contributor.author
Otero, Lisandro Horacio
dc.contributor.author
Song, Wei
dc.contributor.author
Suckow, Mark A.
dc.contributor.author
Schroeder, Valerie A.
dc.contributor.author
Wolter, William R.
dc.contributor.author
Lastochkin, Elena
dc.contributor.author
Antunes, Nuno T.
dc.contributor.author
Pi, Hualiang
dc.contributor.author
Vakulenko, Sergei
dc.contributor.author
Hermoso, Juan Antonio
dc.contributor.author
Chang, Mayland
dc.contributor.author
Mobashery, Shahriar
dc.date.available
2017-04-21T20:28:25Z
dc.date.issued
2015-02
dc.identifier.citation
Bouley, Renee; Kumarasiri, Malika; Peng, Zhihong; Otero, Lisandro Horacio; Song, Wei; et al.; Discovery of antibiotic (E)-3-(3-carboxyphenyl)-2-(4-cyanostyryl)quinazolin-4(3H)-one; American Chemical Society; Journal Of The American Chemical Society; 137; 5; 2-2015; 1738-1741
dc.identifier.uri
http://hdl.handle.net/11336/15602
dc.description.abstract
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.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
American Chemical Society
dc.rights
info:eu-repo/semantics/restrictedAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
Staphylococcus Aureus (Mrsa)
dc.subject
Antiobiotic Resistance
dc.subject
Pbp2a
dc.subject
Quinazolinone
dc.subject.classification
Bioquímica y Biología Molecular
dc.subject.classification
Ciencias Biológicas
dc.subject.classification
CIENCIAS NATURALES Y EXACTAS
dc.title
Discovery of antibiotic (E)-3-(3-carboxyphenyl)-2-(4-cyanostyryl)quinazolin-4(3H)-one
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2016-12-16T17:25:17Z
dc.identifier.eissn
1520-5126
dc.journal.volume
137
dc.journal.number
5
dc.journal.pagination
1738-1741
dc.journal.pais
Estados Unidos
dc.journal.ciudad
Washington
dc.description.fil
Fil: Bouley, Renee. University Of Notre Dame-indiana; Estados Unidos
dc.description.fil
Fil: Kumarasiri, Malika. University Of Notre Dame-indiana; Estados Unidos
dc.description.fil
Fil: Peng, Zhihong. University Of Notre Dame-indiana; Estados Unidos
dc.description.fil
Fil: Otero, Lisandro Horacio. Consejo Superior de Investigaciones Cientificas. Instituto de Quimica Fisica; España. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Pque. Centenario. Instituto de Investigaciones Bioquímicas de Buenos Aires. Fundación Instituto Leloir. Instituto de Investigaciones Bioquímicas de Buenos Aires; Argentina
dc.description.fil
Fil: Song, Wei. University Of Notre Dame-indiana; Estados Unidos
dc.description.fil
Fil: Suckow, Mark A.. University Of Notre Dame-indiana; Estados Unidos
dc.description.fil
Fil: Schroeder, Valerie A.. University Of Notre Dame-indiana; Estados Unidos
dc.description.fil
Fil: Wolter, William R.. University Of Notre Dame-indiana; Estados Unidos
dc.description.fil
Fil: Lastochkin, Elena. University Of Notre Dame-indiana; Estados Unidos
dc.description.fil
Fil: Antunes, Nuno T.. University Of Notre Dame-indiana; Estados Unidos
dc.description.fil
Fil: Pi, Hualiang. University Of Notre Dame-indiana; Estados Unidos
dc.description.fil
Fil: Vakulenko, Sergei. University Of Notre Dame-indiana; Estados Unidos
dc.description.fil
Fil: Hermoso, Juan Antonio. Consejo Superior de Investigaciones Cientificas. Instituto de Quimica Fisica; España
dc.description.fil
Fil: Chang, Mayland. University Of Notre Dame-indiana; Estados Unidos
dc.description.fil
Fil: Mobashery, Shahriar. University Of Notre Dame-indiana; Estados Unidos
dc.journal.title
Journal Of The American Chemical Society
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/http://pubs.acs.org/doi/abs/10.1021/jacs.5b00056
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1021/jacs.5b00056


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