Discovery of a new class of non-â-lactam inhibitors of penicillin-binding proteins with Gram-positive antibacterial activity and oral bioavailability

Autores
O’Daniel, Peter I.; Peng, Zhihong; Pi, Hualiang; Testero, Sebastian Andres; Ding, Derong; Spink, Edward; Leemans, Erika J.; Boudreau, Marc A.; Yamaguchi, Takao; Schroeder, Valerie A; Wolter, William R.; Llarrull, Leticia Irene; Song, Wei; Lashtochkin, Elena; Shi, Qicun; Kumarasiri, Malika; Antunes, Nuno T.; Espahbodi, Mana; Lichtenwalter, Katerina; Suckow, Mark A.; Vakulenko, Sergei; Mobashery, Shahriar; Chang, Mayland
Año de publicación
2014
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
Infections caused by hard-to-treat methicillin-resistantStaphylococcus aureus(MRSA) are a serious global public-health concern,as MRSA has become broadly resistant to many classes of antibiotics. Wedisclose herein the discovery of a new class of non-β-lactam antibiotics,the oxadiazoles, which inhibit penicillin-binding protein 2a (PBP2a) ofMRSA. The oxadiazoles show bactericidal activity against vancomycin-and linezolid-resistant MRSA and other Gram-positive bacterial strains,invivoefficacy in a mouse model of infection, and have 100% oralbioavailability.
Fil: O’Daniel, Peter I.. University of Notre Dame; Estados Unidos
Fil: Peng, Zhihong. University of Notre Dame; Estados Unidos
Fil: Pi, Hualiang. University of Notre Dame; Estados Unidos
Fil: Testero, Sebastian Andres. University of Notre Dame; Estados Unidos. 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
Fil: Ding, Derong. University of Notre Dame; Estados Unidos
Fil: Spink, Edward. University of Notre Dame; Estados Unidos
Fil: Leemans, Erika J.. University of Notre Dame; Estados Unidos
Fil: Boudreau, Marc A.. University of Notre Dame; Estados Unidos
Fil: Yamaguchi, Takao. University of Notre Dame; Estados Unidos
Fil: Schroeder, Valerie A. University of Notre Dame; Estados Unidos
Fil: Wolter, William R.. University of Notre Dame; Estados Unidos
Fil: Llarrull, Leticia Irene. University of Notre Dame; Estados Unidos. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Biología Molecular y Celular de Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Biología Molecular y Celular de Rosario; Argentina
Fil: Song, Wei. University of Notre Dame; Estados Unidos
Fil: Lashtochkin, Elena. University of Notre Dame; Estados Unidos
Fil: Shi, Qicun. University of Notre Dame; Estados Unidos
Fil: Kumarasiri, Malika. University of Notre Dame; Estados Unidos
Fil: Antunes, Nuno T.. University of Notre Dame; Estados Unidos
Fil: Espahbodi, Mana. University of Notre Dame; Estados Unidos
Fil: Lichtenwalter, Katerina. University of Notre Dame; Estados Unidos
Fil: Suckow, Mark A.. University of Notre Dame; Estados Unidos
Fil: Vakulenko, Sergei. University of Notre Dame; Estados Unidos
Fil: Mobashery, Shahriar. University of Notre Dame; Estados Unidos
Fil: Chang, Mayland. University of Notre Dame; Estados Unidos
Materia
Antibiotics
Mrsa
Oxadiazoles
Penicillin Binding Proteins
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/31218
Acceder
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oai_identifier_str oai:ri.conicet.gov.ar:11336/31218
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Discovery of a new class of non-â-lactam inhibitors of penicillin-binding proteins with Gram-positive antibacterial activity and oral bioavailabilityO’Daniel, Peter I.Peng, ZhihongPi, HualiangTestero, Sebastian AndresDing, DerongSpink, EdwardLeemans, Erika J.Boudreau, Marc A.Yamaguchi, TakaoSchroeder, Valerie AWolter, William R.Llarrull, Leticia IreneSong, WeiLashtochkin, ElenaShi, QicunKumarasiri, MalikaAntunes, Nuno T.Espahbodi, ManaLichtenwalter, KaterinaSuckow, Mark A.Vakulenko, SergeiMobashery, ShahriarChang, MaylandAntibioticsMrsaOxadiazolesPenicillin Binding Proteinshttps://purl.org/becyt/ford/1.4https://purl.org/becyt/ford/1Infections caused by hard-to-treat methicillin-resistantStaphylococcus aureus(MRSA) are a serious global public-health concern,as MRSA has become broadly resistant to many classes of antibiotics. Wedisclose herein the discovery of a new class of non-β-lactam antibiotics,the oxadiazoles, which inhibit penicillin-binding protein 2a (PBP2a) ofMRSA. The oxadiazoles show bactericidal activity against vancomycin-and linezolid-resistant MRSA and other Gram-positive bacterial strains,invivoefficacy in a mouse model of infection, and have 100% oralbioavailability.Fil: O’Daniel, Peter I.. University of Notre Dame; Estados UnidosFil: Peng, Zhihong. University of Notre Dame; Estados UnidosFil: Pi, Hualiang. University of Notre Dame; Estados UnidosFil: Testero, Sebastian Andres. University of Notre Dame; Estados Unidos. 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; ArgentinaFil: Ding, Derong. University of Notre Dame; Estados UnidosFil: Spink, Edward. University of Notre Dame; Estados UnidosFil: Leemans, Erika J.. University of Notre Dame; Estados UnidosFil: Boudreau, Marc A.. University of Notre Dame; Estados UnidosFil: Yamaguchi, Takao. University of Notre Dame; Estados UnidosFil: Schroeder, Valerie A. University of Notre Dame; Estados UnidosFil: Wolter, William R.. University of Notre Dame; Estados UnidosFil: Llarrull, Leticia Irene. University of Notre Dame; Estados Unidos. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Biología Molecular y Celular de Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Biología Molecular y Celular de Rosario; ArgentinaFil: Song, Wei. University of Notre Dame; Estados UnidosFil: Lashtochkin, Elena. University of Notre Dame; Estados UnidosFil: Shi, Qicun. University of Notre Dame; Estados UnidosFil: Kumarasiri, Malika. University of Notre Dame; Estados UnidosFil: Antunes, Nuno T.. University of Notre Dame; Estados UnidosFil: Espahbodi, Mana. University of Notre Dame; Estados UnidosFil: Lichtenwalter, Katerina. University of Notre Dame; Estados UnidosFil: Suckow, Mark A.. University of Notre Dame; Estados UnidosFil: Vakulenko, Sergei. University of Notre Dame; Estados UnidosFil: Mobashery, Shahriar. University of Notre Dame; Estados UnidosFil: Chang, Mayland. University of Notre Dame; Estados UnidosAmerican Chemical Society2014-02info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/31218O’Daniel, Peter I.; Peng, Zhihong; Pi, Hualiang; Testero, Sebastian Andres; Ding, Derong; et al.; Discovery of a new class of non-â-lactam inhibitors of penicillin-binding proteins with Gram-positive antibacterial activity and oral bioavailability; American Chemical Society; Journal of the American Chemical Society; 136; 2-2014; 3664-36720002-7863CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/doi/10.1021/ja500053xinfo:eu-repo/semantics/altIdentifier/url/http://pubs.acs.org/doi/10.1021/ja500053xinfo:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-03T09:49:53Zoai:ri.conicet.gov.ar:11336/31218instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-09-03 09:49:54.661CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Discovery of a new class of non-â-lactam inhibitors of penicillin-binding proteins with Gram-positive antibacterial activity and oral bioavailability
title Discovery of a new class of non-â-lactam inhibitors of penicillin-binding proteins with Gram-positive antibacterial activity and oral bioavailability
spellingShingle Discovery of a new class of non-â-lactam inhibitors of penicillin-binding proteins with Gram-positive antibacterial activity and oral bioavailability
O’Daniel, Peter I.
Antibiotics
Mrsa
Oxadiazoles
Penicillin Binding Proteins
title_short Discovery of a new class of non-â-lactam inhibitors of penicillin-binding proteins with Gram-positive antibacterial activity and oral bioavailability
title_full Discovery of a new class of non-â-lactam inhibitors of penicillin-binding proteins with Gram-positive antibacterial activity and oral bioavailability
title_fullStr Discovery of a new class of non-â-lactam inhibitors of penicillin-binding proteins with Gram-positive antibacterial activity and oral bioavailability
title_full_unstemmed Discovery of a new class of non-â-lactam inhibitors of penicillin-binding proteins with Gram-positive antibacterial activity and oral bioavailability
title_sort Discovery of a new class of non-â-lactam inhibitors of penicillin-binding proteins with Gram-positive antibacterial activity and oral bioavailability
dc.creator.none.fl_str_mv O’Daniel, Peter I.
Peng, Zhihong
Pi, Hualiang
Testero, Sebastian Andres
Ding, Derong
Spink, Edward
Leemans, Erika J.
Boudreau, Marc A.
Yamaguchi, Takao
Schroeder, Valerie A
Wolter, William R.
Llarrull, Leticia Irene
Song, Wei
Lashtochkin, Elena
Shi, Qicun
Kumarasiri, Malika
Antunes, Nuno T.
Espahbodi, Mana
Lichtenwalter, Katerina
Suckow, Mark A.
Vakulenko, Sergei
Mobashery, Shahriar
Chang, Mayland
author O’Daniel, Peter I.
author_facet O’Daniel, Peter I.
Peng, Zhihong
Pi, Hualiang
Testero, Sebastian Andres
Ding, Derong
Spink, Edward
Leemans, Erika J.
Boudreau, Marc A.
Yamaguchi, Takao
Schroeder, Valerie A
Wolter, William R.
Llarrull, Leticia Irene
Song, Wei
Lashtochkin, Elena
Shi, Qicun
Kumarasiri, Malika
Antunes, Nuno T.
Espahbodi, Mana
Lichtenwalter, Katerina
Suckow, Mark A.
Vakulenko, Sergei
Mobashery, Shahriar
Chang, Mayland
author_role author
author2 Peng, Zhihong
Pi, Hualiang
Testero, Sebastian Andres
Ding, Derong
Spink, Edward
Leemans, Erika J.
Boudreau, Marc A.
Yamaguchi, Takao
Schroeder, Valerie A
Wolter, William R.
Llarrull, Leticia Irene
Song, Wei
Lashtochkin, Elena
Shi, Qicun
Kumarasiri, Malika
Antunes, Nuno T.
Espahbodi, Mana
Lichtenwalter, Katerina
Suckow, Mark A.
Vakulenko, Sergei
Mobashery, Shahriar
Chang, Mayland
author2_role author
author
author
author
author
author
author
author
author
author
author
author
author
author
author
author
author
author
author
author
author
author
dc.subject.none.fl_str_mv Antibiotics
Mrsa
Oxadiazoles
Penicillin Binding Proteins
topic Antibiotics
Mrsa
Oxadiazoles
Penicillin Binding Proteins
purl_subject.fl_str_mv https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
dc.description.none.fl_txt_mv Infections caused by hard-to-treat methicillin-resistantStaphylococcus aureus(MRSA) are a serious global public-health concern,as MRSA has become broadly resistant to many classes of antibiotics. Wedisclose herein the discovery of a new class of non-β-lactam antibiotics,the oxadiazoles, which inhibit penicillin-binding protein 2a (PBP2a) ofMRSA. The oxadiazoles show bactericidal activity against vancomycin-and linezolid-resistant MRSA and other Gram-positive bacterial strains,invivoefficacy in a mouse model of infection, and have 100% oralbioavailability.
Fil: O’Daniel, Peter I.. University of Notre Dame; Estados Unidos
Fil: Peng, Zhihong. University of Notre Dame; Estados Unidos
Fil: Pi, Hualiang. University of Notre Dame; Estados Unidos
Fil: Testero, Sebastian Andres. University of Notre Dame; Estados Unidos. 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
Fil: Ding, Derong. University of Notre Dame; Estados Unidos
Fil: Spink, Edward. University of Notre Dame; Estados Unidos
Fil: Leemans, Erika J.. University of Notre Dame; Estados Unidos
Fil: Boudreau, Marc A.. University of Notre Dame; Estados Unidos
Fil: Yamaguchi, Takao. University of Notre Dame; Estados Unidos
Fil: Schroeder, Valerie A. University of Notre Dame; Estados Unidos
Fil: Wolter, William R.. University of Notre Dame; Estados Unidos
Fil: Llarrull, Leticia Irene. University of Notre Dame; Estados Unidos. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario. Instituto de Biología Molecular y Celular de Rosario. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Instituto de Biología Molecular y Celular de Rosario; Argentina
Fil: Song, Wei. University of Notre Dame; Estados Unidos
Fil: Lashtochkin, Elena. University of Notre Dame; Estados Unidos
Fil: Shi, Qicun. University of Notre Dame; Estados Unidos
Fil: Kumarasiri, Malika. University of Notre Dame; Estados Unidos
Fil: Antunes, Nuno T.. University of Notre Dame; Estados Unidos
Fil: Espahbodi, Mana. University of Notre Dame; Estados Unidos
Fil: Lichtenwalter, Katerina. University of Notre Dame; Estados Unidos
Fil: Suckow, Mark A.. University of Notre Dame; Estados Unidos
Fil: Vakulenko, Sergei. University of Notre Dame; Estados Unidos
Fil: Mobashery, Shahriar. University of Notre Dame; Estados Unidos
Fil: Chang, Mayland. University of Notre Dame; Estados Unidos
description Infections caused by hard-to-treat methicillin-resistantStaphylococcus aureus(MRSA) are a serious global public-health concern,as MRSA has become broadly resistant to many classes of antibiotics. Wedisclose herein the discovery of a new class of non-β-lactam antibiotics,the oxadiazoles, which inhibit penicillin-binding protein 2a (PBP2a) ofMRSA. The oxadiazoles show bactericidal activity against vancomycin-and linezolid-resistant MRSA and other Gram-positive bacterial strains,invivoefficacy in a mouse model of infection, and have 100% oralbioavailability.
publishDate 2014
dc.date.none.fl_str_mv 2014-02
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/31218
O’Daniel, Peter I.; Peng, Zhihong; Pi, Hualiang; Testero, Sebastian Andres; Ding, Derong; et al.; Discovery of a new class of non-â-lactam inhibitors of penicillin-binding proteins with Gram-positive antibacterial activity and oral bioavailability; American Chemical Society; Journal of the American Chemical Society; 136; 2-2014; 3664-3672
0002-7863
CONICET Digital
CONICET
url http://hdl.handle.net/11336/31218
identifier_str_mv O’Daniel, Peter I.; Peng, Zhihong; Pi, Hualiang; Testero, Sebastian Andres; Ding, Derong; et al.; Discovery of a new class of non-â-lactam inhibitors of penicillin-binding proteins with Gram-positive antibacterial activity and oral bioavailability; American Chemical Society; Journal of the American Chemical Society; 136; 2-2014; 3664-3672
0002-7863
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/doi/10.1021/ja500053x
info:eu-repo/semantics/altIdentifier/url/http://pubs.acs.org/doi/10.1021/ja500053x
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
application/pdf
dc.publisher.none.fl_str_mv American Chemical Society
publisher.none.fl_str_mv American Chemical Society
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
repository.name.fl_str_mv CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
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score 13.13397

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