SrasV1, Main, Exploration, bibRecord, 002357

Structure-activity relationships study of 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives as novel non-nucleoside anti-hepatitis B virus agents

Identifieur interne : 002357 ( Main/Exploration ); précédent : 002356; suivant : 002358

Structure-activity relationships study of 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives as novel non-nucleoside anti-hepatitis B virus agents

Auteurs : Rui-Hua Guo [République populaire de Chine] ; QUAN ZHANG [République populaire de Chine] ; Yun-Bao Ma [République populaire de Chine] ; JIE LUO [République populaire de Chine] ; Chang-An Geng [République populaire de Chine] ; Li-Jun Wang [République populaire de Chine] ; Xue-Mei Zhang [République populaire de Chine] ; JUN ZHOU [République populaire de Chine] ; Zhi-Yong Jiang [République populaire de Chine] ; Ji-Jun Chen [République populaire de Chine]

Source :

European journal of medicinal chemistry [ 0223-5234 ] ; 2011.

RBID : Pascal:11-0310569

Descripteurs français

Pascal (Inist)
- Relation structure activité, Composé non nucléoside, Antiviral, Virus hépatite B, Synthèse chimique, Dérivé du benzène, Hétérocycle azote, Composé bicyclique, Composé aromatique, In vitro, Mécanisme action, Lactame, Quinoléin-2-one dérivé, Cinnamique acid(3-méthoxy) ester 2-[6-chloro-4-(2-chlorophényl)-1,2-dihydro-2-oxo-3-quinolyl]éthyle.

English descriptors

KwdEn :
- Antiviral, Aromatic compound, Benzene derivatives, Bicyclic compound, Chemical synthesis, Hepatitis B virus, In vitro, Lactam, Mechanism of action, Nitrogen heterocycle, Non nucleoside compound, Structure activity relation.

Abstract

A series of novel 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives were synthesized and evaluated for anti-hepatitis B virus (anti-HBV) activities in vitro to explore their structure-activity relationships (SARs). Most of the synthesized compounds possessed potent anti-HBV activity, of which the promising compound 44 exhibited significantly inhibitory potency against the secretion of hepatitis surface antigen (HBsAg) (IC₅₀ = 0.010 mM, SI > 135), hepatitis e antigen (HBeAg) (IC₅₀ = 0.026 mM, SI > 51) and the replication of HBV DNA (IC₅₀ = 0.045 mM). Preliminary mechanism study suggested compound 44 could mainly enhance the transcript activity of HBV ENI (enhancer I), EN-II (enhancer II).

Affiliations:

Links toward previous steps (curation, corpus...)

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Le document en format XML

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</inist:fA14>
<country>République populaire de Chine</country>
<wicri:noRegion>Kunming 650204</wicri:noRegion>
</affiliation>
</author>
<author><name sortKey="Chen, Ji Jun" sort="Chen, Ji Jun" uniqKey="Chen J" first="Ji-Jun" last="Chen">Ji-Jun Chen</name>
<affiliation wicri:level="1"><inist:fA14 i1="01"><s1>State Key Laboratory of Photochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences</s1>
<s2>Kunming 650204</s2>
<s3>CHN</s3>
<sZ>1 aut.</sZ>
<sZ>2 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>5 aut.</sZ>
<sZ>6 aut.</sZ>
<sZ>7 aut.</sZ>
<sZ>8 aut.</sZ>
<sZ>9 aut.</sZ>
<sZ>10 aut.</sZ>
</inist:fA14>
<country>République populaire de Chine</country>
<wicri:noRegion>Kunming 650204</wicri:noRegion>
</affiliation>
</author>
</analytic>
<series><title level="j" type="main">European journal of medicinal chemistry</title>
<title level="j" type="abbreviated">Eur. j. med. chem.</title>
<idno type="ISSN">0223-5234</idno>
<imprint><date when="2011">2011</date>
</imprint>
</series>
</biblStruct>
</sourceDesc>
<seriesStmt><title level="j" type="main">European journal of medicinal chemistry</title>
<title level="j" type="abbreviated">Eur. j. med. chem.</title>
<idno type="ISSN">0223-5234</idno>
</seriesStmt>
</fileDesc>
<profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Antiviral</term>
<term>Aromatic compound</term>
<term>Benzene derivatives</term>
<term>Bicyclic compound</term>
<term>Chemical synthesis</term>
<term>Hepatitis B virus</term>
<term>In vitro</term>
<term>Lactam</term>
<term>Mechanism of action</term>
<term>Nitrogen heterocycle</term>
<term>Non nucleoside compound</term>
<term>Structure activity relation</term>
</keywords>
<keywords scheme="Pascal" xml:lang="fr"><term>Relation structure activité</term>
<term>Composé non nucléoside</term>
<term>Antiviral</term>
<term>Virus hépatite B</term>
<term>Synthèse chimique</term>
<term>Dérivé du benzène</term>
<term>Hétérocycle azote</term>
<term>Composé bicyclique</term>
<term>Composé aromatique</term>
<term>In vitro</term>
<term>Mécanisme action</term>
<term>Lactame</term>
<term>Quinoléin-2-one dérivé</term>
<term>Cinnamique acid(3-méthoxy) ester 2-[6-chloro-4-(2-chlorophényl)-1,2-dihydro-2-oxo-3-quinolyl]éthyle</term>
</keywords>
</textClass>
</profileDesc>
</teiHeader>
<front><div type="abstract" xml:lang="en">A series of novel 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives were synthesized and evaluated for anti-hepatitis B virus (anti-HBV) activities in vitro to explore their structure-activity relationships (SARs). Most of the synthesized compounds possessed potent anti-HBV activity, of which the promising compound 44 exhibited significantly inhibitory potency against the secretion of hepatitis surface antigen (HBsAg) (IC<sub>50</sub>
 = 0.010 mM, SI > 135), hepatitis e antigen (HBeAg) (IC<sub>50</sub>
 = 0.026 mM, SI > 51) and the replication of HBV DNA (IC<sub>50</sub>
 = 0.045 mM). Preliminary mechanism study suggested compound 44 could mainly enhance the transcript activity of HBV ENI (enhancer I), EN-II (enhancer II).</div>
</front>
</TEI>
<affiliations><list><country><li>République populaire de Chine</li>
</country>
<settlement><li>Pékin</li>
</settlement>
</list>
<tree><country name="République populaire de Chine"><noRegion><name sortKey="Guo, Rui Hua" sort="Guo, Rui Hua" uniqKey="Guo R" first="Rui-Hua" last="Guo">Rui-Hua Guo</name>
</noRegion>
<name sortKey="Chen, Ji Jun" sort="Chen, Ji Jun" uniqKey="Chen J" first="Ji-Jun" last="Chen">Ji-Jun Chen</name>
<name sortKey="Geng, Chang An" sort="Geng, Chang An" uniqKey="Geng C" first="Chang-An" last="Geng">Chang-An Geng</name>
<name sortKey="Geng, Chang An" sort="Geng, Chang An" uniqKey="Geng C" first="Chang-An" last="Geng">Chang-An Geng</name>
<name sortKey="Guo, Rui Hua" sort="Guo, Rui Hua" uniqKey="Guo R" first="Rui-Hua" last="Guo">Rui-Hua Guo</name>
<name sortKey="Jiang, Zhi Yong" sort="Jiang, Zhi Yong" uniqKey="Jiang Z" first="Zhi-Yong" last="Jiang">Zhi-Yong Jiang</name>
<name sortKey="Jie Luo" sort="Jie Luo" uniqKey="Jie Luo" last="Jie Luo">JIE LUO</name>
<name sortKey="Jun Zhou" sort="Jun Zhou" uniqKey="Jun Zhou" last="Jun Zhou">JUN ZHOU</name>
<name sortKey="Ma, Yun Bao" sort="Ma, Yun Bao" uniqKey="Ma Y" first="Yun-Bao" last="Ma">Yun-Bao Ma</name>
<name sortKey="Quan Zhang" sort="Quan Zhang" uniqKey="Quan Zhang" last="Quan Zhang">QUAN ZHANG</name>
<name sortKey="Wang, Li Jun" sort="Wang, Li Jun" uniqKey="Wang L" first="Li-Jun" last="Wang">Li-Jun Wang</name>
<name sortKey="Wang, Li Jun" sort="Wang, Li Jun" uniqKey="Wang L" first="Li-Jun" last="Wang">Li-Jun Wang</name>
<name sortKey="Zhang, Xue Mei" sort="Zhang, Xue Mei" uniqKey="Zhang X" first="Xue-Mei" last="Zhang">Xue-Mei Zhang</name>
</country>
</tree>
</affiliations>
</record>

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Structure-activity relationships study of 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives as novel non-nucleoside anti-hepatitis B virus agents

Structure-activity relationships study of 6-chloro-4-(2-chlorophenyl)-3-(2-hydroxyethyl) quinolin-2(1H)-one derivatives as novel non-nucleoside anti-hepatitis B virus agents

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