Mostrar el registro sencillo del ítem
dc.contributor.author
Boudreau, Marc A.
dc.contributor.author
Ding, Derong
dc.contributor.author
Meisel, Jayda E.
dc.contributor.author
Janardhanan, Jeshina
dc.contributor.author
Spink, Edward
dc.contributor.author
Peng, Zhihong
dc.contributor.author
Qian, Yuanyuan
dc.contributor.author
Yamaguchi, Takao
dc.contributor.author
Testero, Sebastian Andres
dc.contributor.author
O'Daniel, Peter I.
dc.contributor.author
Leemans, Erika
dc.contributor.author
Lastochkin, Elena
dc.contributor.author
Song, Wei
dc.contributor.author
Schroeder, Valerie A.
dc.contributor.author
Wolter, William R.
dc.contributor.author
Suckow, Mark A.
dc.contributor.author
Mobashery, Shahriar
dc.contributor.author
Chang, Mayland
dc.date.available
2020-10-28T20:53:53Z
dc.date.issued
2020-03
dc.identifier.citation
Boudreau, Marc A.; Ding, Derong; Meisel, Jayda E.; Janardhanan, Jeshina; Spink, Edward; et al.; Structure-Activity Relationship for the Oxadiazole Class of Antibacterials; American Chemical Society; ACS Medicinal Chemistry Letters; 11; 3; 3-2020; 322-326
dc.identifier.issn
1948-5875
dc.identifier.uri
http://hdl.handle.net/11336/117105
dc.description.abstract
A structure-activity relationship (SAR) for the oxadiazole class of antibacterials was evaluated by syntheses of 72 analogs and determination of the minimal-inhibitory concentrations (MICs) against the ESKAPE panel of bacteria. Selected compounds were further evaluated for in vitro toxicity, plasma protein binding, pharmacokinetics (PK), and a mouse model of methicillin-resistant Staphylococcus aureus (MRSA) infection. Oxadiazole 72c shows potent in vitro antibacterial activity, exhibits low clearance, a high volume of distribution, and 41% oral bioavailability, and shows efficacy in mouse models of MRSA infection.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
American Chemical Society
dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by/2.5/ar/
dc.subject
ANTIBACTERIALS
dc.subject
OXADIAZOLES
dc.subject
PENICILLIN-BINDING PROTEINS
dc.subject
STRUCTURE-ACTIVITY RELATIONSHIP
dc.subject.classification
Química Orgánica
dc.subject.classification
Ciencias Químicas
dc.subject.classification
CIENCIAS NATURALES Y EXACTAS
dc.title
Structure-Activity Relationship for the Oxadiazole Class of Antibacterials
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2020-06-23T15:18:35Z
dc.journal.volume
11
dc.journal.number
3
dc.journal.pagination
322-326
dc.journal.pais
Estados Unidos
dc.journal.ciudad
Washington DC
dc.description.fil
Fil: Boudreau, Marc A.. University of Notre Dame; Estados Unidos
dc.description.fil
Fil: Ding, Derong. University of Notre Dame; Estados Unidos
dc.description.fil
Fil: Meisel, Jayda E.. University of Notre Dame; Estados Unidos
dc.description.fil
Fil: Janardhanan, Jeshina. University of Notre Dame; Estados Unidos
dc.description.fil
Fil: Spink, Edward. University of Notre Dame; Estados Unidos
dc.description.fil
Fil: Peng, Zhihong. University of Notre Dame; Estados Unidos
dc.description.fil
Fil: Qian, Yuanyuan. University of Notre Dame; Estados Unidos
dc.description.fil
Fil: Yamaguchi, Takao. University of Notre Dame; Estados Unidos
dc.description.fil
Fil: Testero, Sebastian Andres. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Química Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Química Rosario; Argentina. University of Notre Dame; Estados Unidos
dc.description.fil
Fil: O'Daniel, Peter I.. University of Notre Dame; Estados Unidos
dc.description.fil
Fil: Leemans, Erika. University of Notre Dame; Estados Unidos
dc.description.fil
Fil: Lastochkin, Elena. University of Notre Dame; Estados Unidos
dc.description.fil
Fil: Song, Wei. University of Notre Dame; Estados Unidos
dc.description.fil
Fil: Schroeder, Valerie A.. University of Notre Dame; Estados Unidos
dc.description.fil
Fil: Wolter, William R.. University of Notre Dame; Estados Unidos
dc.description.fil
Fil: Suckow, Mark A.. University of Notre Dame; Estados Unidos
dc.description.fil
Fil: Mobashery, Shahriar. University of Notre Dame; Estados Unidos
dc.description.fil
Fil: Chang, Mayland. University of Notre Dame; Estados Unidos
dc.journal.title
ACS Medicinal Chemistry Letters
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/http://pubs.acs.org/doi/10.1021/acsmedchemlett.9b00379
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1021/acsmedchemlett.9b00379
Archivos asociados
Tamaño:
595.3Kb
Formato:
PDF