Identification of a new class of HBV capsid assembly modulator.

Antiviral Agents / chemistry Capsid Proteins / antagonists & inhibitors Dose-Response Relationship, Drug Hepatitis B virus / drug effects Microbial Sensitivity Tests Molecular Structure Piperidines / chemistry Pyrazoles / chemistry Structure-Activity Relationship
Capsid HBV Modulator Urea

Journal

Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377

Informations de publication

Date de publication:
01 05 2021
Historique:
received: 12 11 2020
revised: 25 01 2021
accepted: 26 01 2021
pubmed: 22 2 2021
medline: 2 9 2021
entrez: 21 2 2021
Statut: ppublish

Résumé

The HBV core protein is a druggable target of interest due to the multiple essential functions in the HBV life cycle to enable chronic HBV infection. The core protein oligomerizes to form the viral capsid, and modulation of the HBV capsid assembly has shown efficacy in clinical trials. Herein is described the identification and hit to lead SAR of a novel series of pyrazolo piperidine HBV capsid assembly modulators.

Identifiants

DOI: 10.1016/j.bmcl.2021.127848 PMID: 33610748
pubmed: 33610748
pii: S0960-894X(21)00074-3
doi: 10.1016/j.bmcl.2021.127848
pii:
doi:

Substances chimiques

Antiviral Agents 0
Capsid Proteins 0
Piperidines 0
Pyrazoles 0
pyrazole 3QD5KJZ7ZJ
piperidine 67I85E138Y

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

127848

Informations de copyright

Copyright © 2021 Elsevier Ltd. All rights reserved.

Auteurs

Scott D Kuduk (SD)

Novira Therapeutics, a Janssen Pharmaceuticals Company, 1400 McKean Road, Spring House, PA 19477, United States. Electronic address: skuduk@its.jnj.com.

Bart Stoops (B)

Janssen Pharmaceutica, N. V. Turnhoutseweg 30, 2340 Beerse, Belgium.

Richard Alexander (R)

Janssen Research and Development, 1400 McKean Road, Spring House, PA 19477, United States.

Angela M Lam (AM)

Novira Therapeutics, a Janssen Pharmaceuticals Company, 1400 McKean Road, Spring House, PA 19477, United States.

Christine Espiritu (C)

Novira Therapeutics, a Janssen Pharmaceuticals Company, 1400 McKean Road, Spring House, PA 19477, United States.

Robert Vogel (R)

Novira Therapeutics, a Janssen Pharmaceuticals Company, 1400 McKean Road, Spring House, PA 19477, United States.

Vincent Lau (V)

Novira Therapeutics, a Janssen Pharmaceuticals Company, 1400 McKean Road, Spring House, PA 19477, United States.

Klaus Klumpp (K)

Novira Therapeutics, a Janssen Pharmaceuticals Company, 1400 McKean Road, Spring House, PA 19477, United States.

Osvaldo A Flores (OA)

Novira Therapeutics, a Janssen Pharmaceuticals Company, 1400 McKean Road, Spring House, PA 19477, United States.

George D Hartman (GD)

Novira Therapeutics, a Janssen Pharmaceuticals Company, 1400 McKean Road, Spring House, PA 19477, United States.

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Classifications MeSH

questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Anti-infectieux › Antiviraux › Identification of a new class of HBV capsid...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines virales › Protéines virales structurales › Protéines nucléocapside › Protéines de capside › Identification of a new class of HBV capsid...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes toxicologiques › Relation dose-effet des médicaments › Identification of a new class of HBV capsid...
questionsmedicales.fr › Virus › Virus de l'hépatite › Hepadnaviridae › Orthohepadnavirus › Virus de l'hépatite B › Identification of a new class of HBV capsid...
questionsmedicales.fr › Techniques d'investigation › Évaluation préclinique de médicament › Tests de sensibilité microbienne › Identification of a new class of HBV capsid...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Identification of a new class of HBV capsid...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Pipéridines › Identification of a new class of HBV capsid...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Azoles › Pyrazoles › Identification of a new class of HBV capsid...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Identification of a new class of HBV capsid...