1463501-50-9Relevant academic research and scientific papers
Discovery of ANT3310, a Novel Broad-Spectrum Serine β-Lactamase Inhibitor of the Diazabicyclooctane Class, Which Strongly Potentiates Meropenem Activity against Carbapenem-Resistant Enterobacterales and Acinetobacter baumannii
Davies, David T.,Leiris, Simon,Zalacain, Magdalena,Sprynski, Nicolas,Castandet, Jér?me,Bousquet, Justine,Lozano, Clarisse,Llanos, Agustina,Alibaud, Laethitia,Vasa, Srinivas,Pattipati, Ramesh,Valige, Ravindar,Kummari, Bhaskar,Pothukanuri, Srinivasu,De Piano, Cyntia,Morrissey, Ian,Holden, Kirsty,Warn, Peter,Marcoccia, Francesca,Benvenuti, Manuela,Pozzi, Cecilia,Tassone, Giusy,Mangani, Stefano,Docquier, Jean-Denis,Pallin, David,Elliot, Richard,Lemonnier, Marc,Everett, Martin
, p. 15802 - 15820 (2020)
The diazabicyclooctanes (DBOs) are a class of serine β-lactamase (SBL) inhibitors that use a strained urea moiety as the warhead to react with the active serine residue in the active site of SBLs. The first in-class drug, avibactam, as well as several other recently approved DBOs (e.g., relebactam) or those in clinical development (e.g., nacubactam and zidebactam) potentiate activity of β-lactam antibiotics, to various extents, against carbapenem-resistant Enterobacterales (CRE) carrying class A, C, and D SBLs; however, none of these are able to rescue the activity of β-lactam antibiotics against carbapenem-resistant Acinetobacter baumannii (CRAB), a WHO "critical priority pathogen"producing class D OXA-type SBLs. Herein, we describe the chemical optimization and resulting structure-activity relationship, leading to the discovery of a novel DBO, ANT3310, which uniquely has a fluorine atom replacing the carboxamide and stands apart from the current DBOs in restoring carbapenem activity against OXA-CRAB as well as SBL-carrying CRE pathogens.
DIAAZABICYCLOOCTANONE DERIVATIVES AS ANTIBACTERIALS
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, (2020/02/25)
The invention relates to a compound which is a diazabicyclooctanone of Formula (I) or a pharmaceutically acceptable salt thereof: wherein R is as defined herein. The compounds are useful in the treatment of bacterial infection, in particular they are useful in reducing bacterial resistance to antibiotics. They are also useful in the treatment of bacteria which express serine-P-lactamase enzymes, in combination with antibiotics.
A PROCESS FOR PREPARATION OF SODIUM (2S, 5R)-6-(BENZYLOXY)-7-OXO-1,6-DIAZABICYCLO[3.2.1]OCTANE-2-CARBOXYLATE
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, (2015/10/05)
A process for preparation of a compound of Formula (I) is disclosed.
1,2,4-OXADIAZOLE AND 1,2,4-THIADIAZOLE BETA-LACTAMASE INHIBITORS
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, (2013/11/06)
β-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D β-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
BETA-LACTAMASE INHIBITORS
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, (2013/11/19)
Aryl substituted diazabicyclooctanes (DBO) compounds that inhibit β-lactamases of class A, class C or class D and potentiate β-lactam antibiotics are disclosed. In particular, this disclosure provides DBO compounds that, when used in the disclosed Synergy MIC Assay with a β-lactam antibiotic at a fixed concentration have an MIC of 8 μg/mL or less against one or more isogenic β-lactamase expressing bacterial strains.
ISOXAZOLE β-LACTAMASE INHIBITORS
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, (2013/10/21)
β-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D β-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
