Discovery of highly potent and selective influenza virus neuraminidase inhibitors targeting 150-cavity.

Animals Antiviral Agents / chemical synthesis Dose-Response Relationship, Drug Drug Discovery Enzyme Inhibitors / chemical synthesis Female Male Mice Mice, Inbred Strains Microbial Sensitivity Tests Molecular Structure Neuraminidase / antagonists & inhibitors Orthomyxoviridae / drug effects Oseltamivir / analogs & derivatives Structure-Activity Relationship
150-Cavity Influenza virus Neuraminidase inhibitors Oseltamivir derivatives

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:
15 Feb 2021
Historique:
received: 19 08 2020
revised: 08 12 2020
accepted: 08 12 2020
pubmed: 2 1 2021
medline: 24 4 2021
entrez: 1 1 2021
Statut: ppublish

Résumé

Encouraged by our earlier discovery of N1-selective inhibitors, the 150-cavity of influenza virus neuraminidases (NAs) could be further exploited to yield more potent oseltamivir derivatives. Herein, we report the design, synthesis and biological evaluation of a series of novel oseltamivir derivatives via the structural modifications at C

Identifiants

DOI: 10.1016/j.ejmech.2020.113097 PMID: 33385836
pubmed: 33385836
pii: S0223-5234(20)31069-2
doi: 10.1016/j.ejmech.2020.113097
pii:
doi:

Substances chimiques

Antiviral Agents 0
Enzyme Inhibitors 0
Oseltamivir 20O93L6F9H
Neuraminidase EC 3.2.1.18

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

113097

Informations de copyright

Copyright © 2020 Elsevier Masson SAS. All rights reserved.

Déclaration de conflit d'intérêts

Declaration of competing interest The authors declare no conflict of interest.

Auteurs

Ruifang Jia (R)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, 250012, Jinan, Shandong, PR China.

Jian Zhang (J)

Institute of Medical Sciences, The Second Hospital, Cheeloo College of Medicine, Shandong University, 250033, PR China.

Chiara Bertagnin (C)

Department of Molecular Medicine, University of Padova, via Gabelli 63, 35121, Padova, Italy.

Srinivasulu Cherukupalli (S)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, 250012, Jinan, Shandong, PR China.

Wei Ai (W)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, 250012, Jinan, Shandong, PR China.

Xiao Ding (X)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, 250012, Jinan, Shandong, PR China.

Zhuo Li (Z)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, 250012, Jinan, Shandong, PR China.

Jiwei Zhang (J)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, 250012, Jinan, Shandong, PR China.

Han Ju (H)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, 250012, Jinan, Shandong, PR China.

Xiuli Ma (X)

Institute of Poultry Science, Shandong Academy of Agricultural Sciences, 1 Jiaoxiao Road, Jinan, Shandong, 250023, PR China.

Arianna Loregian (A)

Department of Molecular Medicine, University of Padova, via Gabelli 63, 35121, Padova, Italy.

Bing Huang (B)

Institute of Poultry Science, Shandong Academy of Agricultural Sciences, 1 Jiaoxiao Road, Jinan, Shandong, 250023, PR China. Electronic address: hbind@163.com.

Peng Zhan (P)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, 250012, Jinan, Shandong, PR China; China-Belgium Collaborative Research Center for Innovative Antiviral Drugs of Shandong Province, 44 West Culture Road, 250012, Jinan, Shandong, PR China. Electronic address: zhanpeng1982@sdu.edu.cn.

Xinyong Liu (X)

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Cheeloo College of Medicine, Shandong University, 44 West Culture Road, 250012, Jinan, Shandong, PR China; China-Belgium Collaborative Research Center for Innovative Antiviral Drugs of Shandong Province, 44 West Culture Road, 250012, Jinan, Shandong, PR China. Electronic address: xinyongl@sdu.edu.cn.

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Discovery of highly potent and selective...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Anti-infectieux › Antiviraux › Discovery of highly potent and selective...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes toxicologiques › Relation dose-effet des médicaments › Discovery of highly potent and selective...
questionsmedicales.fr › Techniques d'investigation › Développement de médicament › Découverte de médicament › Discovery of highly potent and selective...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Discovery of highly potent and selective...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Discovery of highly potent and selective...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Lignées consanguines de souris › Discovery of highly potent and selective...
questionsmedicales.fr › Techniques d'investigation › Évaluation préclinique de médicament › Tests de sensibilité microbienne › Discovery of highly potent and selective...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Discovery of highly potent and selective...
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Hydrolases › Glycosidases › Sialidase › Discovery of highly potent and selective...
questionsmedicales.fr › Virus › Virus à ARN › Virus à ARN de polarité négative › Orthomyxoviridae › Discovery of highly potent and selective...
questionsmedicales.fr › Composés chimiques organiques › Hydrocarbures › Hydrocarbures cycliques › Hydrocarbures alicycliques › Cyclohexanes › Cyclohexènes › Oséltamivir › Discovery of highly potent and selective...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Discovery of highly potent and selective...