SAR Studies Leading to the Identification of a Novel Series of Metallo-β-lactamase Inhibitors for the Treatment of Carbapenem-Resistant Enterobacteriaceae Infections That Display Efficacy in an Animal Infection Model.
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Authors
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Leiris, Simon1
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Coelho, Alicia1
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Castandet, Jérôme1
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Bayet, Maëlle1
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Lozano, Clarisse1
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Bougnon, Juliette1
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Bousquet, Justine1
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Everett, Martin1
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Lemonnier, Marc1
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Sprynski, Nicolas1
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Zalacain, Magdalena1, 2
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Pallin, Thomas David3
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Cramp, Michael C3
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Jennings, Neil3
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Raphy, Gilles3
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Jones, Mark W3
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Pattipati, Ramesh4
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Shankar, Battu4
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Sivasubrahmanyam, Relangi4
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Soodhagani, Ashok K4
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Juventhala, Ramakrishna R4
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Pottabathini, Narender4
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Pothukanuri, Srinivasu4
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Benvenuti, Manuela5
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Pozzi, Cecilia5
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Mangani, Stefano5
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De Luca, Filomena6
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Cerboni, Giulia6
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Docquier, Jean-Denis6
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Davies, David T1
And 10 more
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1
Antabio SAS , 436 rue Pierre et Marie Curie , 31670 Labège , France.
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(France)
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2
Zala Drug Discovery Consulting LLC , West Chester , Pennsylvania 19380 , United States.
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(United States)
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3
Charles River Laboratories , 8-9 The Spire Green Centre , Harlow CM19 5TR , United Kingdom.
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(United Kingdom)
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4
GVK Biosciences Private Limited , Plot No. 28 A , IDA Nacharam , Hyderabad 500076 , India.
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(India)
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5
Department of Biotechnology, Chemistry and Pharmacy , University of Siena , 2 Via Aldo Moro , Siena , 53100 Italy.
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(Italy)
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6
Department of Medical Biotechnology , University of Siena , 16 Viale Bracci , Siena , 53100 Italy.
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(Italy)
- Type
- Published Article
- Journal
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ACS Infectious Diseases
- Publisher
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American Chemical Society
- Publication Date
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Nov 30, 2018
- Identifiers
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DOI: 10.1021/acsinfecdis.8b00246
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PMID: 30427656
- Source
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Medline
- Keywords
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- Language
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English
- License
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Unknown
Abstract
The clinical effectiveness of carbapenem antibiotics such as meropenem is becoming increasingly compromised by the spread of both metallo-β-lactamase (MBL) and serine-β-lactamase (SBL) enzymes on mobile genetic elements, stimulating research to find new β-lactamase inhibitors to be used in conjunction with carbapenems and other β-lactam antibiotics. Herein, we describe our initial exploration of a novel chemical series of metallo-β-lactamase inhibitors, from concept to efficacy, in a survival model using an advanced tool compound (ANT431) in conjunction with meropenem.
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
This record was last updated on 10/20/2019 and may not reflect the most current and accurate biomedical/scientific data available from NLM.
The corresponding record at NLM can be accessed at
https://www.ncbi.nlm.nih.gov/pubmed/30427656
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