Discovery of a novel, highly potent and orally bioavailable pyrrolidinone indole series of irreversible Myeloperoxidase (MPO) inhibitors.

Rats Mice Animals Dogs Peroxidase Hydrogen Peroxide Cardiovascular Diseases Antioxidants Indoles Pyrrolidinones
Indole Irreversible inhibitor MPO Mechanism-based inhibitor Myeloperoxidase Peroxidase

Journal

Biochemical pharmacology
ISSN: 1873-2968
Titre abrégé: Biochem Pharmacol
Pays: England
ID NLM: 0101032

Informations de publication

Date de publication:
03 2023
Historique:
received: 22 08 2022
revised: 13 01 2023
accepted: 17 01 2023
pubmed: 25 1 2023
medline: 15 3 2023
entrez: 24 1 2023
Statut: ppublish

Résumé

Myeloperoxidase (MPO) is a heme-containing peroxidase from phagocytic cells, which plays an important role in the innate immune response. The primary anti-microbial function of MPO is achieved by catalyzing the oxidation of halides by hydrogen peroxide (H

Identifiants

DOI: 10.1016/j.bcp.2023.115418 PMID: 36693437
pubmed: 36693437
pii: S0006-2952(23)00009-6
doi: 10.1016/j.bcp.2023.115418
pii:
doi:

Substances chimiques

Peroxidase EC 1.11.1.7
Hydrogen Peroxide BBX060AN9V
Antioxidants 0
Indoles 0
Pyrrolidinones 0

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

115418

Informations de copyright

Copyright © 2023 Elsevier Inc. All rights reserved.

Déclaration de conflit d'intérêts

Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Auteurs

Jean B Regard (JB)

Cardiovascular and Metabolic Diseases, Cambridge, MA, USA.

Tyler J Harrison (TJ)

Global Discovery Chemistry, Cambridge, MA, USA.

Jake Axford (J)

Global Discovery Chemistry, Cambridge, MA, USA.

Laura Axford (L)

Cardiovascular and Metabolic Diseases, Cambridge, MA, USA. Electronic address: laura.axford@novartis.com.

Lac Lee (L)

Cardiovascular and Metabolic Diseases, Cambridge, MA, USA.

Xianglin Ren (X)

Cardiovascular and Metabolic Diseases, Cambridge, MA, USA.

Lin Deng (L)

PK Sciences, Cambridge, MA, USA.

Aimee Reynolds (A)

Technical R&D, Cambridge, MA, USA.

Justin Mao (J)

Global Discovery Chemistry, Cambridge, MA, USA.

Qian Liu (Q)

Global Discovery Chemistry, Cambridge, MA, USA.

Anup Patnaik (A)

Global Discovery Chemistry, Cambridge, MA, USA.

Evan Cohick (E)

Cardiovascular and Metabolic Diseases, Cambridge, MA, USA.

Micah Hollis-Symynkywicz (M)

Cardiovascular and Metabolic Diseases, Cambridge, MA, USA.

Sally Loi (S)

Cardiovascular and Metabolic Diseases, Cambridge, MA, USA.

Simone Riek (S)

Novartis Institutes for BioMedical Research, Autoimmunity, Transplantation and Inflammation, Switzlerland.

Una McKeever (U)

Novartis Institutes for BioMedical Research, Autoimmunity, Transplantation and Inflammation, Switzlerland.

David Dunstan (D)

Global Discovery Chemistry, Cambridge, MA, USA.

MooJe Sung (M)

Global Discovery Chemistry, Cambridge, MA, USA.

Nathaniel F Ware (NF)

Global Discovery Chemistry, Cambridge, MA, USA.

Alan P Brown (AP)

Preclinical Safety, Novartis Institutes for BioMedical Research, Fabrikstrasse 2 Novartis Campus, Basel CH-4056, Switzerland.

Lawrence G Hamann (LG)

Global Discovery Chemistry, Cambridge, MA, USA.

Jovita Marcinkeviciene (J)

Cardiovascular and Metabolic Diseases, Cambridge, MA, USA.

Andrew W Patterson (AW)

Global Discovery Chemistry, Cambridge, MA, USA.

Martin L Marro (ML)

Cardiovascular and Metabolic Diseases, Cambridge, MA, USA.

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Rats › Discovery of a novel, highly potent and orally...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Discovery of a novel, highly potent and orally...
questionsmedicales.fr › Eucaryotes › Animaux › Discovery of a novel, highly potent and orally...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Carnivora › Pinnipedia › Canidae › Chiens › Discovery of a novel, highly potent and orally...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Oxidoreductases › Peroxidases › Myeloperoxidase › Discovery of a novel, highly potent and orally...
questionsmedicales.fr › Composés chimiques organiques › Radicaux libres › Peroxydes › Peroxyde d'hydrogène › Discovery of a novel, highly potent and orally...
questionsmedicales.fr › Maladies cardiovasculaires › Discovery of a novel, highly potent and orally...
questionsmedicales.fr › Actions chimiques et utilisations › Utilisations spécialisées de produits chimiques › Agents protecteurs › Antioxydants › Discovery of a novel, highly potent and orally...
questionsmedicales.fr › Composés hétérocycliques › Composés hétérocycliques à cycles fusionnés › Composés hétérobicycliques › Indoles › Discovery of a novel, highly potent and orally...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Pyrrolidines › Pyrrolidones › Discovery of a novel, highly potent and orally...