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Discovery of a New Class of Non-β-lactam Inhibitors of Penicillin-Binding Proteins with Gram-Positive Antibacterial Activity
[Image: see text] Infections caused by hard-to-treat methicillin-resistant Staphylococcus aureus (MRSA) are a serious global public-health concern, as MRSA has become broadly resistant to many classes of antibiotics. We disclose herein the discovery of a new class of non-β-lactam antibiotics, the ox...
| Autores principales: | , , , , , , , , , , , , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
American Chemical
Society
2014
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| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3985699/ https://www.ncbi.nlm.nih.gov/pubmed/24517363 http://dx.doi.org/10.1021/ja500053x |
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| author | O’Daniel, Peter I. Peng, Zhihong Pi, Hualiang Testero, Sebastian A. Ding, Derong Spink, Edward Leemans, Erika Boudreau, Marc A. Yamaguchi, Takao Schroeder, Valerie A. Wolter, William R. Llarrull, Leticia I. Song, Wei Lastochkin, Elena Kumarasiri, Malika Antunes, Nuno T. Espahbodi, Mana Lichtenwalter, Katerina Suckow, Mark A. Vakulenko, Sergei Mobashery, Shahriar Chang, Mayland |
| author_facet | O’Daniel, Peter I. Peng, Zhihong Pi, Hualiang Testero, Sebastian A. Ding, Derong Spink, Edward Leemans, Erika Boudreau, Marc A. Yamaguchi, Takao Schroeder, Valerie A. Wolter, William R. Llarrull, Leticia I. Song, Wei Lastochkin, Elena Kumarasiri, Malika Antunes, Nuno T. Espahbodi, Mana Lichtenwalter, Katerina Suckow, Mark A. Vakulenko, Sergei Mobashery, Shahriar Chang, Mayland |
| author_sort | O’Daniel, Peter I. |
| collection | PubMed |
| description | [Image: see text] Infections caused by hard-to-treat methicillin-resistant Staphylococcus aureus (MRSA) are a serious global public-health concern, as MRSA has become broadly resistant to many classes of antibiotics. We disclose herein the discovery of a new class of non-β-lactam antibiotics, the oxadiazoles, which inhibit penicillin-binding protein 2a (PBP2a) of MRSA. The oxadiazoles show bactericidal activity against vancomycin- and linezolid-resistant MRSA and other Gram-positive bacterial strains, in vivo efficacy in a mouse model of infection, and have 100% oral bioavailability. |
| format | Online Article Text |
| id | pubmed-3985699 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2014 |
| publisher | American Chemical
Society |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-39856992015-02-11 Discovery of a New Class of Non-β-lactam Inhibitors of Penicillin-Binding Proteins with Gram-Positive Antibacterial Activity O’Daniel, Peter I. Peng, Zhihong Pi, Hualiang Testero, Sebastian A. Ding, Derong Spink, Edward Leemans, Erika Boudreau, Marc A. Yamaguchi, Takao Schroeder, Valerie A. Wolter, William R. Llarrull, Leticia I. Song, Wei Lastochkin, Elena Kumarasiri, Malika Antunes, Nuno T. Espahbodi, Mana Lichtenwalter, Katerina Suckow, Mark A. Vakulenko, Sergei Mobashery, Shahriar Chang, Mayland J Am Chem Soc [Image: see text] Infections caused by hard-to-treat methicillin-resistant Staphylococcus aureus (MRSA) are a serious global public-health concern, as MRSA has become broadly resistant to many classes of antibiotics. We disclose herein the discovery of a new class of non-β-lactam antibiotics, the oxadiazoles, which inhibit penicillin-binding protein 2a (PBP2a) of MRSA. The oxadiazoles show bactericidal activity against vancomycin- and linezolid-resistant MRSA and other Gram-positive bacterial strains, in vivo efficacy in a mouse model of infection, and have 100% oral bioavailability. American Chemical Society 2014-02-11 2014-03-05 /pmc/articles/PMC3985699/ /pubmed/24517363 http://dx.doi.org/10.1021/ja500053x Text en Copyright © 2014 American Chemical Society |
| spellingShingle | O’Daniel, Peter I. Peng, Zhihong Pi, Hualiang Testero, Sebastian A. Ding, Derong Spink, Edward Leemans, Erika Boudreau, Marc A. Yamaguchi, Takao Schroeder, Valerie A. Wolter, William R. Llarrull, Leticia I. Song, Wei Lastochkin, Elena Kumarasiri, Malika Antunes, Nuno T. Espahbodi, Mana Lichtenwalter, Katerina Suckow, Mark A. Vakulenko, Sergei Mobashery, Shahriar Chang, Mayland Discovery of a New Class of Non-β-lactam Inhibitors of Penicillin-Binding Proteins with Gram-Positive Antibacterial Activity |
| title | Discovery
of a New Class of Non-β-lactam Inhibitors
of Penicillin-Binding Proteins with Gram-Positive Antibacterial Activity |
| title_full | Discovery
of a New Class of Non-β-lactam Inhibitors
of Penicillin-Binding Proteins with Gram-Positive Antibacterial Activity |
| title_fullStr | Discovery
of a New Class of Non-β-lactam Inhibitors
of Penicillin-Binding Proteins with Gram-Positive Antibacterial Activity |
| title_full_unstemmed | Discovery
of a New Class of Non-β-lactam Inhibitors
of Penicillin-Binding Proteins with Gram-Positive Antibacterial Activity |
| title_short | Discovery
of a New Class of Non-β-lactam Inhibitors
of Penicillin-Binding Proteins with Gram-Positive Antibacterial Activity |
| title_sort | discovery
of a new class of non-β-lactam inhibitors
of penicillin-binding proteins with gram-positive antibacterial activity |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3985699/ https://www.ncbi.nlm.nih.gov/pubmed/24517363 http://dx.doi.org/10.1021/ja500053x |
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