SrasV1, PascalFrancis, Corpus, bibRecord, 000607

Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors

Identifieur interne : 000607 ( PascalFrancis/Corpus ); précédent : 000606; suivant : 000608

Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors

Auteurs : Li-Rung Chen ; Yu-Chin Wang ; YI WEN LIN ; Shan-Yen Chou ; Shyh-Fong Chen ; LEE TAI LIU ; Ying-Ta Wu ; Chih-Jung Kuo ; Tom Shieh-Shung Chen ; Shin-Hun Juang

Source :

Bioorganic & medicinal chemistry letters : (Print) [ 0960-894X ] ; 2005.

RBID : Pascal:05-0412561

Descripteurs français

Pascal (Inist)
- Synthèse chimique, Isatine, Virus syndrome respiratoire aigu sévère, Inhibiteur protease, Activité biologique, In vitro, Sélectivité, Peptidases, Antiviral, Modèle moléculaire, Complexe enzyme inhibiteur, Indole dérivé, Inhibiteur enzyme, Modélisation, Indole-2,3-dione(1-[benzo[b]thién-2-ylméthyl]-5-iodo), Benzo[b]thiophène dérivé, benzothiophene.

English descriptors

KwdEn :
- Antiviral, Biological activity, Chemical synthesis, Enzyme inhibitor, In vitro, Indole derivatives, Inhibitor enzyme complex, Modeling, Molecular model, Peptidases, Protease inhibitor, Selectivity, Severe acute respiratory syndrome virus.

Abstract

N-Substituted isatin derivatives were prepared from the reaction of isatin and various bromides via two steps. Bioactivity assay results (in vitro tests) demonstrated that some of these compounds are potent and selective inhibitors against SARS coronavirus 3CL protease with IC₅₀ values ranging from 0.95 to 17.50 μM. Additionally, isatin 4o exhibited more potent inhibition for SARS coronavirus protease than for other proteases including papain, chymotrypsin, and trypsin.

Notice en format standard (ISO 2709)

Pour connaître la documentation sur le format Inist Standard.

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A03		`1`		`@0 Bioorg. med. chem. lett. : (Print)`
A05				`@2 15`
A06				`@2 12`
A08	`01`	`1`	`ENG`	`@1 Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors`
A11	`01`	`1`		`@1 CHEN (Li-Rung)`
A11	`02`	`1`		`@1 WANG (Yu-Chin)`
A11	`03`	`1`		`@1 YI WEN LIN`
A11	`04`	`1`		`@1 CHOU (Shan-Yen)`
A11	`05`	`1`		`@1 CHEN (Shyh-Fong)`
A11	`06`	`1`		`@1 LEE TAI LIU`
A11	`07`	`1`		`@1 WU (Ying-Ta)`
A11	`08`	`1`		`@1 KUO (Chih-Jung)`
A11	`09`	`1`		`@1 CHEN (Tom Shieh-Shung)`
A11	`10`	`1`		`@1 JUANG (Shin-Hun)`
A14	`01`			`@1 Development Center for Biotechnology, 102, Lane 169, Kang Ning St @2 Xi Zhi 221, Taipei @3 TWN @Z 1 aut. @Z 2 aut. @Z 3 aut. @Z 4 aut. @Z 5 aut. @Z 6 aut. @Z 9 aut. @Z 10 aut.`
A14	`02`			`@1 Institute of Biological Chemistry and the Genomic Research Center, Academia Sinica @2 Nang Gang 11529, Taipei @3 TWN @Z 7 aut. @Z 8 aut.`
A20				`@1 3058-3062`
A21				`@1 2005`
A23	`01`			`@0 ENG`
A43	`01`			`@1 INIST @2 22446 @5 354000138092570220`
A44				`@0 0000 @1 © 2005 INIST-CNRS. All rights reserved.`
A47	`01`	`1`		`@0 05-0412561`
A60				`@1 P`
A61				`@0 A`
A64	`01`	`1`		`@0 Bioorganic & medicinal chemistry letters : (Print)`
A66	`01`			`@0 GBR`
A99				`@0 3/4 p. ref. et notes`
C01	`01`		`ENG`	`@0 N-Substituted isatin derivatives were prepared from the reaction of isatin and various bromides via two steps. Bioactivity assay results (in vitro tests) demonstrated that some of these compounds are potent and selective inhibitors against SARS coronavirus 3CL protease with IC₅₀ values ranging from 0.95 to 17.50 μM. Additionally, isatin 4o exhibited more potent inhibition for SARS coronavirus protease than for other proteases including papain, chymotrypsin, and trypsin.`
C02	`01`	`X`		`@0 002B02S05`
C03	`01`	`X`	`FRE`	`@0 Synthèse chimique @5 01`
C03	`01`	`X`	`ENG`	`@0 Chemical synthesis @5 01`
C03	`01`	`X`	`SPA`	`@0 Síntesis química @5 01`
C03	`02`	`X`	`FRE`	`@0 Isatine @2 NK @2 FR @5 02`
C03	`03`	`X`	`FRE`	`@0 Virus syndrome respiratoire aigu sévère @2 NW @5 03`
C03	`03`	`X`	`ENG`	`@0 Severe acute respiratory syndrome virus @2 NW @5 03`
C03	`03`	`X`	`SPA`	`@0 Severe acute respiratory syndrome virus @2 NW @5 03`
C03	`04`	`X`	`FRE`	`@0 Inhibiteur protease @2 FR @5 04`
C03	`04`	`X`	`ENG`	`@0 Protease inhibitor @2 FR @5 04`
C03	`04`	`X`	`SPA`	`@0 Inhibidor proteasa @2 FR @5 04`
C03	`05`	`X`	`FRE`	`@0 Activité biologique @5 05`
C03	`05`	`X`	`ENG`	`@0 Biological activity @5 05`
C03	`05`	`X`	`SPA`	`@0 Actividad biológica @5 05`
C03	`06`	`X`	`FRE`	`@0 In vitro @5 06`
C03	`06`	`X`	`ENG`	`@0 In vitro @5 06`
C03	`06`	`X`	`SPA`	`@0 In vitro @5 06`
C03	`07`	`X`	`FRE`	`@0 Sélectivité @5 07`
C03	`07`	`X`	`ENG`	`@0 Selectivity @5 07`
C03	`07`	`X`	`SPA`	`@0 Selectividad @5 07`
C03	`08`	`X`	`FRE`	`@0 Peptidases @2 FE @5 08`
C03	`08`	`X`	`ENG`	`@0 Peptidases @2 FE @5 08`
C03	`08`	`X`	`SPA`	`@0 Peptidases @2 FE @5 08`
C03	`09`	`X`	`FRE`	`@0 Antiviral @5 09`
C03	`09`	`X`	`ENG`	`@0 Antiviral @5 09`
C03	`09`	`X`	`SPA`	`@0 Antiviral @5 09`
C03	`10`	`X`	`FRE`	`@0 Modèle moléculaire @5 10`
C03	`10`	`X`	`ENG`	`@0 Molecular model @5 10`
C03	`10`	`X`	`SPA`	`@0 Modelo molecular @5 10`
C03	`11`	`X`	`FRE`	`@0 Complexe enzyme inhibiteur @5 11`
C03	`11`	`X`	`ENG`	`@0 Inhibitor enzyme complex @5 11`
C03	`11`	`X`	`SPA`	`@0 Complejo enzima inhibidor @5 11`
C03	`12`	`X`	`FRE`	`@0 Indole dérivé @5 32`
C03	`12`	`X`	`ENG`	`@0 Indole derivatives @5 32`
C03	`12`	`X`	`SPA`	`@0 Indol derivado @5 32`
C03	`13`	`X`	`FRE`	`@0 Inhibiteur enzyme @5 33`
C03	`13`	`X`	`ENG`	`@0 Enzyme inhibitor @5 33`
C03	`13`	`X`	`SPA`	`@0 Inhibidor enzima @5 33`
C03	`14`	`X`	`FRE`	`@0 Modélisation @5 34`
C03	`14`	`X`	`ENG`	`@0 Modeling @5 34`
C03	`14`	`X`	`SPA`	`@0 Modelización @5 34`
C03	`15`	`X`	`FRE`	`@0 Indole-2,3-dione(1-[benzo[b]thién-2-ylméthyl]-5-iodo) @2 NK @2 FR @4 INC @5 76`
C03	`16`	`X`	`FRE`	`@0 Benzo[b]thiophène dérivé @2 NK @4 INC @5 77`
C03	`17`	`X`	`FRE`	`@0 benzothiophene @4 INC @5 78`
C07	`01`	`X`	`FRE`	`@0 Coronavirus @2 NW`
C07	`01`	`X`	`ENG`	`@0 Coronavirus @2 NW`
C07	`01`	`X`	`SPA`	`@0 Coronavirus @2 NW`
C07	`02`	`X`	`FRE`	`@0 Coronaviridae @2 NW`
C07	`02`	`X`	`ENG`	`@0 Coronaviridae @2 NW`
C07	`02`	`X`	`SPA`	`@0 Coronaviridae @2 NW`
C07	`03`	`X`	`FRE`	`@0 Nidovirales @2 NW`
C07	`03`	`X`	`ENG`	`@0 Nidovirales @2 NW`
C07	`03`	`X`	`SPA`	`@0 Nidovirales @2 NW`
C07	`04`	`X`	`FRE`	`@0 Virus @2 NW`
C07	`04`	`X`	`ENG`	`@0 Virus @2 NW`
C07	`04`	`X`	`SPA`	`@0 Virus @2 NW`
C07	`05`	`X`	`FRE`	`@0 Hydrolases @2 FE`
C07	`05`	`X`	`ENG`	`@0 Hydrolases @2 FE`
C07	`05`	`X`	`SPA`	`@0 Hydrolases @2 FE`
C07	`06`	`X`	`FRE`	`@0 Enzyme @2 FE`
C07	`06`	`X`	`ENG`	`@0 Enzyme @2 FE`
C07	`06`	`X`	`SPA`	`@0 Enzima @2 FE`
N21				`@1 290`

Format Inist (serveur)

NO :	PASCAL 05-0412561 INIST
ET :	Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors
AU :	CHEN (Li-Rung); WANG (Yu-Chin); YI WEN LIN; CHOU (Shan-Yen); CHEN (Shyh-Fong); LEE TAI LIU; WU (Ying-Ta); KUO (Chih-Jung); CHEN (Tom Shieh-Shung); JUANG (Shin-Hun)
AF :	Development Center for Biotechnology, 102, Lane 169, Kang Ning St/Xi Zhi 221, Taipei/Taïwan (1 aut., 2 aut., 3 aut., 4 aut., 5 aut., 6 aut., 9 aut., 10 aut.); Institute of Biological Chemistry and the Genomic Research Center, Academia Sinica/Nang Gang 11529, Taipei/Taïwan (7 aut., 8 aut.)
DT :	Publication en série; Niveau analytique
SO :	Bioorganic & medicinal chemistry letters : (Print); ISSN 0960-894X; Royaume-Uni; Da. 2005; Vol. 15; No. 12; Pp. 3058-3062
LA :	Anglais
EA :	N-Substituted isatin derivatives were prepared from the reaction of isatin and various bromides via two steps. Bioactivity assay results (in vitro tests) demonstrated that some of these compounds are potent and selective inhibitors against SARS coronavirus 3CL protease with IC₅₀ values ranging from 0.95 to 17.50 μM. Additionally, isatin 4o exhibited more potent inhibition for SARS coronavirus protease than for other proteases including papain, chymotrypsin, and trypsin.
CC :	002B02S05
FD :	Synthèse chimique; Isatine; Virus syndrome respiratoire aigu sévère; Inhibiteur protease; Activité biologique; In vitro; Sélectivité; Peptidases; Antiviral; Modèle moléculaire; Complexe enzyme inhibiteur; Indole dérivé; Inhibiteur enzyme; Modélisation; Indole-2,3-dione(1-[benzo[b]thién-2-ylméth yl]-5-iodo); Benzo[b]thiophène dérivé; benzothiophene
FG :	Coronavirus; Coronaviridae; Nidovirales; Virus; Hydrolases; Enzyme
ED :	Chemical synthesis; Severe acute respiratory syndrome virus; Protease inhibitor; Biological activity; In vitro; Selectivity; Peptidases; Antiviral; Molecular model; Inhibitor enzyme complex; Indole derivatives; Enzyme inhibitor; Modeling
EG :	Coronavirus; Coronaviridae; Nidovirales; Virus; Hydrolases; Enzyme
SD :	Síntesis química; Severe acute respiratory syndrome virus; Inhibidor proteasa; Actividad biológica; In vitro; Selectividad; Peptidases; Antiviral; Modelo molecular; Complejo enzima inhibidor; Indol derivado; Inhibidor enzima; Modelización
LO :	INIST-22446.354000138092570220
ID :	05-0412561

Links to Exploration step

Pascal:05-0412561

Le document en format XML

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<author><name sortKey="Chen, Tom Shieh Shung" sort="Chen, Tom Shieh Shung" uniqKey="Chen T" first="Tom Shieh-Shung" last="Chen">Tom Shieh-Shung Chen</name>
<affiliation><inist:fA14 i1="01"><s1>Development Center for Biotechnology, 102, Lane 169, Kang Ning St</s1>
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<author><name sortKey="Juang, Shin Hun" sort="Juang, Shin Hun" uniqKey="Juang S" first="Shin-Hun" last="Juang">Shin-Hun Juang</name>
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<series><title level="j" type="main">Bioorganic & medicinal chemistry letters : (Print)</title>
<title level="j" type="abbreviated">Bioorg. med. chem. lett. : (Print)</title>
<idno type="ISSN">0960-894X</idno>
<imprint><date when="2005">2005</date>
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<seriesStmt><title level="j" type="main">Bioorganic & medicinal chemistry letters : (Print)</title>
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<profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Antiviral</term>
<term>Biological activity</term>
<term>Chemical synthesis</term>
<term>Enzyme inhibitor</term>
<term>In vitro</term>
<term>Indole derivatives</term>
<term>Inhibitor enzyme complex</term>
<term>Modeling</term>
<term>Molecular model</term>
<term>Peptidases</term>
<term>Protease inhibitor</term>
<term>Selectivity</term>
<term>Severe acute respiratory syndrome virus</term>
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<keywords scheme="Pascal" xml:lang="fr"><term>Synthèse chimique</term>
<term>Isatine</term>
<term>Virus syndrome respiratoire aigu sévère</term>
<term>Inhibiteur protease</term>
<term>Activité biologique</term>
<term>In vitro</term>
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<term>Indole dérivé</term>
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<term>Indole-2,3-dione(1-[benzo[b]thién-2-ylméthyl]-5-iodo)</term>
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<front><div type="abstract" xml:lang="en">N-Substituted isatin derivatives were prepared from the reaction of isatin and various bromides via two steps. Bioactivity assay results (in vitro tests) demonstrated that some of these compounds are potent and selective inhibitors against SARS coronavirus 3CL protease with IC<sub>50</sub>
 values ranging from 0.95 to 17.50 μM. Additionally, isatin 4o exhibited more potent inhibition for SARS coronavirus protease than for other proteases including papain, chymotrypsin, and trypsin.</div>
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<fC01 i1="01" l="ENG"><s0>N-Substituted isatin derivatives were prepared from the reaction of isatin and various bromides via two steps. Bioactivity assay results (in vitro tests) demonstrated that some of these compounds are potent and selective inhibitors against SARS coronavirus 3CL protease with IC<sub>50</sub>
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<ET>Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors</ET>
<AU>CHEN (Li-Rung); WANG (Yu-Chin); YI WEN LIN; CHOU (Shan-Yen); CHEN (Shyh-Fong); LEE TAI LIU; WU (Ying-Ta); KUO (Chih-Jung); CHEN (Tom Shieh-Shung); JUANG (Shin-Hun)</AU>
<AF>Development Center for Biotechnology, 102, Lane 169, Kang Ning St/Xi Zhi 221, Taipei/Taïwan (1 aut., 2 aut., 3 aut., 4 aut., 5 aut., 6 aut., 9 aut., 10 aut.); Institute of Biological Chemistry and the Genomic Research Center, Academia Sinica/Nang Gang 11529, Taipei/Taïwan (7 aut., 8 aut.)</AF>
<DT>Publication en série; Niveau analytique</DT>
<SO>Bioorganic & medicinal chemistry letters : (Print); ISSN 0960-894X; Royaume-Uni; Da. 2005; Vol. 15; No. 12; Pp. 3058-3062</SO>
<LA>Anglais</LA>
<EA>N-Substituted isatin derivatives were prepared from the reaction of isatin and various bromides via two steps. Bioactivity assay results (in vitro tests) demonstrated that some of these compounds are potent and selective inhibitors against SARS coronavirus 3CL protease with IC<sub>50</sub>
 values ranging from 0.95 to 17.50 μM. Additionally, isatin 4o exhibited more potent inhibition for SARS coronavirus protease than for other proteases including papain, chymotrypsin, and trypsin.</EA>
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<FD>Synthèse chimique; Isatine; Virus syndrome respiratoire aigu sévère; Inhibiteur protease; Activité biologique; In vitro; Sélectivité; Peptidases; Antiviral; Modèle moléculaire; Complexe enzyme inhibiteur; Indole dérivé; Inhibiteur enzyme; Modélisation; Indole-2,3-dione(1-[benzo[b]thién-2-ylméth yl]-5-iodo); Benzo[b]thiophène dérivé; benzothiophene</FD>
<FG>Coronavirus; Coronaviridae; Nidovirales; Virus; Hydrolases; Enzyme</FG>
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<SD>Síntesis química; Severe acute respiratory syndrome virus; Inhibidor proteasa; Actividad biológica; In vitro; Selectividad; Peptidases; Antiviral; Modelo molecular; Complejo enzima inhibidor; Indol derivado; Inhibidor enzima; Modelización</SD>
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Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors

Synthesis and evaluation of isatin derivatives as effective SARS coronavirus 3CL protease inhibitors

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