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.

Simon Leiris; Alicia Coelho; Jérôme Castandet; Maëlle Bayet; Clarisse Lozano; Juliette Bougnon; Justine Bousquet; Martin Everett; Marc Lemonnier; Nicolas Sprynski; Magdalena Zalacain; Thomas David Pallin; Michael C Cramp; Neil Jennings; Gilles Raphy; Mark W Jones; Ramesh Pattipati; Battu Shankar; Relangi Sivasubrahmanyam; Ashok K Soodhagani; Ramakrishna R Juventhala; Narender Pottabathini; Srinivasu Pothukanuri; Manuela Benvenuti; Cecilia Pozzi; Stefano Mangani; Filomena De Luca; Giulia Cerboni; Jean-Denis Docquier; David T Davies

doi:10.1021/acsinfecdis.8b00246

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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, Magdalena^{1, 2}
Pallin, Thomas David³
Cramp, Michael C³
Jennings, Neil³
Raphy, Gilles³
Jones, Mark W³
Pattipati, Ramesh⁴
Shankar, Battu⁴
Sivasubrahmanyam, Relangi⁴
Soodhagani, Ashok K⁴
Juventhala, Ramakrishna R⁴
Pottabathini, Narender⁴
Pothukanuri, Srinivasu⁴
Benvenuti, Manuela⁵
Pozzi, Cecilia⁵
Mangani, Stefano⁵
De Luca, Filomena⁶
Cerboni, Giulia⁶
Docquier, Jean-Denis⁶
Davies, David T¹

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.

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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