Discovery of

Acinetobacter / drug effects Animals Anti-Bacterial Agents / chemistry Binding Sites Carbapenems / pharmacology Drug Evaluation, Preclinical Drug Resistance, Bacterial / drug effects Enterobacteriaceae / drug effects Half-Life Mice Microbial Sensitivity Tests Molecular Docking Simulation Octanes / chemistry Stereoisomerism Structure-Activity Relationship beta-Lactamase Inhibitors / chemistry beta-Lactamases / chemistry

Journal

Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531

Informations de publication

Date de publication:
24 12 2020
Historique:
pubmed: 12 12 2020
medline: 3 2 2021
entrez: 11 12 2020
Statut: ppublish

Résumé

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

Identifiants

DOI: 10.1021/acs.jmedchem.0c01535 PMID: 33306385
pubmed: 33306385
doi: 10.1021/acs.jmedchem.0c01535
doi:

Substances chimiques

Anti-Bacterial Agents 0
Carbapenems 0
Octanes 0
beta-Lactamase Inhibitors 0
beta-Lactamases EC 3.5.2.6

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

15802-15820

Auteurs

David T Davies (DT)

Antabio SAS, 436 rue Pierre et Marie Curie, 31670 Labège, France.
ORCID: 0000-0001-7392-4886

Simon Leiris (S)

Antabio SAS, 436 rue Pierre et Marie Curie, 31670 Labège, France.

Magdalena Zalacain (M)

Antabio SAS, 436 rue Pierre et Marie Curie, 31670 Labège, France.

Nicolas Sprynski (N)

Antabio SAS, 436 rue Pierre et Marie Curie, 31670 Labège, France.
ORCID: 0000-0001-8165-6949

Jérôme Castandet (J)

Antabio SAS, 436 rue Pierre et Marie Curie, 31670 Labège, France.

Justine Bousquet (J)

Antabio SAS, 436 rue Pierre et Marie Curie, 31670 Labège, France.

Clarisse Lozano (C)

Antabio SAS, 436 rue Pierre et Marie Curie, 31670 Labège, France.

Agustina Llanos (A)

Antabio SAS, 436 rue Pierre et Marie Curie, 31670 Labège, France.

Laethitia Alibaud (L)

Antabio SAS, 436 rue Pierre et Marie Curie, 31670 Labège, France.

Srinivas Vasa (S)

GVK Biosciences Pvt. Ltd., Survey No. 125 and 126, IDA, Mallapur, Hyderabad, Telangana 500 076, India.

Ramesh Pattipati (R)

GVK Biosciences Pvt. Ltd., Survey No. 125 and 126, IDA, Mallapur, Hyderabad, Telangana 500 076, India.
ORCID: 0000-0002-9925-2704

Ravindar Valige (R)

GVK Biosciences Pvt. Ltd., Survey No. 125 and 126, IDA, Mallapur, Hyderabad, Telangana 500 076, India.

Bhaskar Kummari (B)

GVK Biosciences Pvt. Ltd., Survey No. 125 and 126, IDA, Mallapur, Hyderabad, Telangana 500 076, India.

Srinivasu Pothukanuri (S)

GVK Biosciences Pvt. Ltd., Survey No. 125 and 126, IDA, Mallapur, Hyderabad, Telangana 500 076, India.
ORCID: 0000-0002-0374-8060

Cyntia De Piano (C)

International Health Management Associates (IHMA), Rte. De I'Ile-au-Bois 1A, 1870 Monthey, Switzerland.

Ian Morrissey (I)

International Health Management Associates (IHMA), Rte. De I'Ile-au-Bois 1A, 1870 Monthey, Switzerland.

Kirsty Holden (K)

Evotec (UK) Ltd., Block 23, Alderley Park, Macclesfield, Cheshire SK10 4TG, U.K.

Peter Warn (P)

Evotec (UK) Ltd., Block 23, Alderley Park, Macclesfield, Cheshire SK10 4TG, U.K.

Francesca Marcoccia (F)

Dipartimento di Biotecnologie Mediche, University of Siena, Viale Bracci 16, Siena 53100, Italy.

Manuela Benvenuti (M)

Dipartimento di Biotecnologie, Chimica e Farmacia, University of Siena, Via Aldo Moro 2, Siena 53100, Italy.
ORCID: 0000-0003-0709-2537

Cecilia Pozzi (C)

Dipartimento di Biotecnologie, Chimica e Farmacia, University of Siena, Via Aldo Moro 2, Siena 53100, Italy.
ORCID: 0000-0003-2574-3911

Giusy Tassone (G)

Dipartimento di Biotecnologie, Chimica e Farmacia, University of Siena, Via Aldo Moro 2, Siena 53100, Italy.
ORCID: 0000-0002-2575-5528

Stefano Mangani (S)

Dipartimento di Biotecnologie, Chimica e Farmacia, University of Siena, Via Aldo Moro 2, Siena 53100, Italy.
ORCID: 0000-0003-4824-7478

Jean-Denis Docquier (JD)

Dipartimento di Biotecnologie Mediche, University of Siena, Viale Bracci 16, Siena 53100, Italy.
ORCID: 0000-0001-9483-4476

David Pallin (D)

Charles River Laboratories, 8-9 The Spire Green Centre, Harlow, Essex CM19 5TR, U.K.
ORCID: 0000-0001-5153-7965

Richard Elliot (R)

Charles River Laboratories, 8-9 The Spire Green Centre, Harlow, Essex CM19 5TR, U.K.

Marc Lemonnier (M)

Antabio SAS, 436 rue Pierre et Marie Curie, 31670 Labège, France.
ORCID: 0000-0002-8587-9864

Martin Everett (M)

Antabio SAS, 436 rue Pierre et Marie Curie, 31670 Labège, France.
ORCID: 0000-0003-2002-1805

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Classifications MeSH

questionsmedicales.fr › Bactéries › Proteobacteria › Gammaproteobacteria › Moraxellaceae › Acinetobacter › Discovery of
questionsmedicales.fr › Eucaryotes › Animaux › Discovery of
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Anti-infectieux › Antibactériens › Discovery of
questionsmedicales.fr › Phénomènes chimiques › Phénomènes biochimiques › Sites de fixation › Discovery of
questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérobicycliques › bêta-Lactames › Carbapénèmes › Discovery of
questionsmedicales.fr › Techniques d'investigation › Évaluation préclinique de médicament › Discovery of
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Résistance aux substances › Résistance microbienne aux médicaments › Résistance bactérienne aux médicaments › Discovery of
questionsmedicales.fr › Bactéries › Proteobacteria › Gammaproteobacteria › Enterobacteriaceae › Discovery of
questionsmedicales.fr › Phénomènes physiques › Temps › Période › Discovery of
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Discovery of
questionsmedicales.fr › Techniques d'investigation › Évaluation préclinique de médicament › Tests de sensibilité microbienne › Discovery of
questionsmedicales.fr › Sciences de l'information › Méthodologies informatiques › Simulation numérique › Simulation de docking moléculaire › Discovery of
questionsmedicales.fr › Composés chimiques organiques › Hydrocarbures › Hydrocarbures acycliques › Alcanes › Octanes › Discovery of
questionsmedicales.fr › Phénomènes chimiques › Phénomènes de chimie organique › Isomérie › Stéréoisomérie › Discovery of
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Discovery of
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Anti-infectieux › Antibactériens › Inhibiteurs des bêta-lactamases › Discovery of
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Hydrolases › Amidohydrolases › bêta-Lactamases › Discovery of