Медицинская библиотека · ACS infectious diseases · 2018

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.

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

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Аннотация

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.

Для цитирования: Leiris Simon, Coelho Alicia, Castandet Jérôme, Bayet Maëlle, Lozano Clarisse, Bougnon Juliette, Bousquet Justine, Everett Martin, Lemonnier Marc, Sprynski Nicolas, Zalacain Magdalena, Pallin Thomas David, Cramp Michael C, Jennings Neil, Raphy Gilles, Jones Mark W, Pattipati Ramesh, Shankar Battu, Sivasubrahmanyam Relangi, Soodhagani Ashok K, Juventhala Ramakrishna R, Pottabathini Narender, Pothukanuri Srinivasu, Benvenuti Manuela, Pozzi Cecilia, Mangani Stefano, De Luca Filomena, Cerboni Giulia, Docquier Jean-Denis, Davies David T. 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.. ACS infectious diseases. 2018. DOI: 10.1021/acsinfecdis.8b00246.

Предметные рубрики MeSH

Anti-Bacterial Agents Carbapenem-Resistant Enterobacteriaceae Carbapenems Crystallography, X-Ray Drug Resistance, Multiple, Bacterial Enterobacteriaceae Infections Inhibitory Concentration 50 Meropenem Microbial Sensitivity Tests Picolinic Acids Protein Binding Structure-Activity Relationship beta-Lactamase Inhibitors beta-Lactamases

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