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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.

Authors
  • Leiris, Simon1
  • Coelho, Alicia1
  • Castandet, Jérôme1
  • Bayet, Maëlle1
  • Lozano, Clarisse1
  • Bougnon, Juliette1
  • Bousquet, Justine1
  • Everett, Martin1
  • Lemonnier, Marc1
  • Sprynski, Nicolas1
  • Zalacain, Magdalena1, 2
  • Pallin, Thomas David3
  • Cramp, Michael C3
  • Jennings, Neil3
  • Raphy, Gilles3
  • Jones, Mark W3
  • Pattipati, Ramesh4
  • Shankar, Battu4
  • Sivasubrahmanyam, Relangi4
  • Soodhagani, Ashok K4
  • And 10 more
  • 1 Antabio SAS , 436 rue Pierre et Marie Curie , 31670 Labège , France. , (France)
  • 2 Zala Drug Discovery Consulting LLC , West Chester , Pennsylvania 19380 , United States. , (United States)
  • 3 Charles River Laboratories , 8-9 The Spire Green Centre , Harlow CM19 5TR , United Kingdom. , (United Kingdom)
  • 4 GVK Biosciences Private Limited , Plot No. 28 A , IDA Nacharam , Hyderabad 500076 , India. , (India)
  • 5 Department of Biotechnology, Chemistry and Pharmacy , University of Siena , 2 Via Aldo Moro , Siena , 53100 Italy. , (Italy)
  • 6 Department of Medical Biotechnology , University of Siena , 16 Viale Bracci , Siena , 53100 Italy. , (Italy)
Type
Published Article
Journal
ACS Infectious Diseases
Publisher
American Chemical Society
Publication Date
Nov 30, 2018
Identifiers
DOI: 10.1021/acsinfecdis.8b00246
PMID: 30427656
Source
Medline
Keywords
Language
English
License
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.

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