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 | Zendy

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

Open Access

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

Author(s) -

Simon Leiris,

Alicia Coelho,

Jérôme Castandet,

Maëlle Bayet,

Clarisse Lozano,

Juliette Boug,

Justine Bousquet,

Martin Everett,

Marc Lemonnier,

Nicolas Sprynski,

Magdalena Zalacaín,

T. David Pallin,

Michael C. Cramp,

Neil Jennings,

Gilles Raphy,

Mark 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,

JeanDenis Docquier,

David T. Davies

Publication year - 2018

Publication title -

acs infectious diseases

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.324

H-Index - 39

ISSN - 2373-8227

DOI - 10.1021/acsinfecdis.8b00246

Subject(s) - meropenem , antibiotics , carbapenem , enterobacteriaceae , carbapenem resistant enterobacteriaceae , microbiology and biotechnology , biology , escherichia coli , antibiotic resistance , gene , genetics

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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