Discovery, optimization and biological evaluation of novel HBsAg production inhibitors.
Anti-HBV
Bridged ring
HBsAg
Synthesis
THP (Tetrahydropyridine)
Journal
European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510
Informations de publication
Date de publication:
05 Aug 2023
05 Aug 2023
Historique:
received:
12
02
2023
revised:
14
04
2023
accepted:
16
04
2023
medline:
2
6
2023
pubmed:
16
5
2023
entrez:
15
5
2023
Statut:
ppublish
Résumé
Hepatitis B virus (HBV) infection is a major global health problem. HBsAg inhibitors are expected to reduce the production of HBsAg via inhibiting host proteins PAPD5 & PAPD7 and finally achieve the ideal goal of "functional cure". In this work, a series of tetrahydropyridine (THP) derivatives with a bridged ring were synthesized and evaluated for their inhibiting HBsAg production and HBV DNA activity. Among them, compound 17i was identified as potent HBsAg production inhibitor with excellent in vitro anti-HBV potency (HBV DNA EC
Identifiants
pubmed: 37187088
pii: S0223-5234(23)00353-7
doi: 10.1016/j.ejmech.2023.115387
pii:
doi:
Substances chimiques
Hepatitis B Surface Antigens
0
DNA, Viral
0
Antiviral Agents
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
115387Informations de copyright
Copyright © 2023 Elsevier Masson SAS. 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.