SrasV1, Main, Exploration, bibRecord, 000D63

Structure-activity relationships of 3-O-β-chacotriosyl oleanic acid derivatives as entry inhibitors for highly pathogenic H5N1 influenza virus.

Identifieur interne : 000D63 ( Main/Exploration ); précédent : 000D62; suivant : 000D64

Structure-activity relationships of 3-O-β-chacotriosyl oleanic acid derivatives as entry inhibitors for highly pathogenic H5N1 influenza virus.

Auteurs : Sumei Li [République populaire de Chine] ; Xiuhua Jia [République populaire de Chine] ; Xintian Shen [République populaire de Chine] ; Zhuwen Wei [République populaire de Chine] ; Zhiyan Jiang [République populaire de Chine] ; Yixian Liao [République populaire de Chine] ; Yiming Guo [République populaire de Chine] ; Xiaojun Zheng [République populaire de Chine] ; Guohua Zhong [République populaire de Chine] ; Gaopeng Song [République populaire de Chine]

Source :

Bioorganic & medicinal chemistry [ 1464-3391 ] ; 2017.

RBID : pubmed:28651913

Descripteurs français

KwdFr :
- Acide oléanolique (), Acide oléanolique (pharmacologie), Acide oléanolique (synthèse chimique), Animaux, Antiviraux (), Antiviraux (pharmacologie), Antiviraux (synthèse chimique), Cellules rénales canines Madin-Darby (), Cellules rénales canines Madin-Darby (virologie), Chiens, Relation dose-effet des médicaments, Relation structure-activité, Sous-type H5N1 du virus de la grippe A (), Structure moléculaire, Tests de sensibilité microbienne.
MESH :
- pharmacologie : Acide oléanolique, Antiviraux.
- synthèse chimique : Acide oléanolique, Antiviraux.
- virologie : Cellules rénales canines Madin-Darby.
- Acide oléanolique, Animaux, Antiviraux, Cellules rénales canines Madin-Darby, Chiens, Relation dose-effet des médicaments, Relation structure-activité, Sous-type H5N1 du virus de la grippe A, Structure moléculaire, Tests de sensibilité microbienne.

English descriptors

KwdEn :
- Animals, Antiviral Agents (chemical synthesis), Antiviral Agents (chemistry), Antiviral Agents (pharmacology), Dogs, Dose-Response Relationship, Drug, Influenza A Virus, H5N1 Subtype (drug effects), Madin Darby Canine Kidney Cells (drug effects), Madin Darby Canine Kidney Cells (virology), Microbial Sensitivity Tests, Molecular Structure, Oleanolic Acid (chemical synthesis), Oleanolic Acid (chemistry), Oleanolic Acid (pharmacology), Structure-Activity Relationship.
MESH :
- chemical , chemical synthesis : Antiviral Agents, Oleanolic Acid.
- chemical , chemistry : Antiviral Agents, Oleanolic Acid.
- chemical , pharmacology : Antiviral Agents, Oleanolic Acid.
- drug effects : Influenza A Virus, H5N1 Subtype, Madin Darby Canine Kidney Cells.
- virology : Madin Darby Canine Kidney Cells.
- Animals, Dogs, Dose-Response Relationship, Drug, Microbial Sensitivity Tests, Molecular Structure, Structure-Activity Relationship.

Abstract

Highly pathogenic H5N1 virus (H5N1) entry is a key target for the development of novel anti-influenza agents with new mechanisms of action. In our continuing efforts to identify novel potential anti-H5N1 entry inhibitors, a series of 3-O-β-chacotriosyl oleanolic acid analogs have been designed, synthesized and evaluated as H5N1 entry inhibitors based on two small molecule inhibitors 1 and 2 previously discovered by us. The anti-H5N1 entry activities were determined based on HA/HIV and VSVG/HIV entry assays. Compound 15 displayed the most promising anti-H5N1 entry activities with average IC₅₀ values of 4.05μM and good selective index (22.9). Detailed structure-activity relationships (SARs) studies suggested that either the introduction of an additional oxo group to position 11 at OA or alteration of the C-3 configuration of OA from 3β- to 3α-forms can significantly enhance the selective index while maintaining their antiviral activities in vitro. Molecular simulation analysis confirmed that the compounds exert their inhibitory activity through binding tightly to hemagglutinin (HA2) protein near the fusion peptide and prevent virus entry.

DOI: 10.1016/j.bmc.2017.06.025
PubMed: 28651913

Affiliations:

Le document en format XML

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<term>Animaux</term>
<term>Antiviraux ()</term>
<term>Antiviraux (pharmacologie)</term>
<term>Antiviraux (synthèse chimique)</term>
<term>Cellules rénales canines Madin-Darby ()</term>
<term>Cellules rénales canines Madin-Darby (virologie)</term>
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<keywords scheme="MESH" type="chemical" qualifier="chemistry" xml:lang="en"><term>Antiviral Agents</term>
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<keywords scheme="MESH" type="chemical" qualifier="pharmacology" xml:lang="en"><term>Antiviral Agents</term>
<term>Oleanolic Acid</term>
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<term>Madin Darby Canine Kidney Cells</term>
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<front><div type="abstract" xml:lang="en">Highly pathogenic H5N1 virus (H5N1) entry is a key target for the development of novel anti-influenza agents with new mechanisms of action. In our continuing efforts to identify novel potential anti-H5N1 entry inhibitors, a series of 3-O-β-chacotriosyl oleanolic acid analogs have been designed, synthesized and evaluated as H5N1 entry inhibitors based on two small molecule inhibitors 1 and 2 previously discovered by us. The anti-H5N1 entry activities were determined based on HA/HIV and VSVG/HIV entry assays. Compound 15 displayed the most promising anti-H5N1 entry activities with average IC<sub>50</sub>
 values of 4.05μM and good selective index (22.9). Detailed structure-activity relationships (SARs) studies suggested that either the introduction of an additional oxo group to position 11 at OA or alteration of the C-3 configuration of OA from 3β- to 3α-forms can significantly enhance the selective index while maintaining their antiviral activities in vitro. Molecular simulation analysis confirmed that the compounds exert their inhibitory activity through binding tightly to hemagglutinin (HA2) protein near the fusion peptide and prevent virus entry.</div>
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</tree>
</affiliations>
</record>

Pour manipuler ce document sous Unix (Dilib)

EXPLOR_STEP=$WICRI_ROOT/Sante/explor/SrasV1/Data/Main/Exploration

HfdSelect -h $EXPLOR_STEP/biblio.hfd -nk 000D63 | SxmlIndent | more

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{{Explor lien
   |wiki=    Sante
   |area=    SrasV1
   |flux=    Main
   |étape=   Exploration
   |type=    RBID
   |clé=     pubmed:28651913
   |texte=   Structure-activity relationships of 3-O-β-chacotriosyl oleanic acid derivatives as entry inhibitors for highly pathogenic H5N1 influenza virus.
}}

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HfdIndexSelect -h $EXPLOR_AREA/Data/Main/Exploration/RBID.i   -Sk "pubmed:28651913" \
       | HfdSelect -Kh $EXPLOR_AREA/Data/Main/Exploration/biblio.hfd   \
       | NlmPubMed2Wicri -a SrasV1

This area was generated with Dilib version V0.6.33.
Data generation: Tue Apr 28 14:49:16 2020. Site generation: Sat Mar 27 22:06:49 2021

Serveur d'exploration SRAS

Structure-activity relationships of 3-O-β-chacotriosyl oleanic acid derivatives as entry inhibitors for highly pathogenic H5N1 influenza virus.

Structure-activity relationships of 3-O-β-chacotriosyl oleanic acid derivatives as entry inhibitors for highly pathogenic H5N1 influenza virus.

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Pour générer des pages wiki

	Serveur d'exploration SRAS
	Attention, ce site est en cours de développement ! Attention, site généré par des moyens informatiques à partir de corpus bruts. Les informations ne sont donc pas validées.