SrasV1, PascalFrancis, Corpus, bibRecord, 000456

Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors

Identifieur interne : 000456 ( PascalFrancis/Corpus ); précédent : 000455; suivant : 000457

Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors

Auteurs : LU ZHOU ; YING LIU ; WEILIN ZHANG ; PING WEI ; CHANGKANG HUANG ; JIANFENG PEI ; YAXIA YUAN ; LUHUA LAI

Source :

Journal of medicinal chemistry : (Print) [ 0022-2623 ] ; 2006.

RBID : Pascal:06-0478361

Descripteurs français

Pascal (Inist)
- Isatine, Virus syndrome respiratoire aigu sévère, Inhibiteur protease, Relation structure activité, In vitro, Sélectivité, Synthèse chimique, Naphtalène dérivé, Carboxamide, Indole dérivé, Peptidases, Inhibiteur enzyme, Antiviral, Indole-5-carboxamide(2,3-dihydro-2,3-dioxo-1-[2-naphtylméthyl]), Liaison non covalente.

English descriptors

KwdEn :
- Antiviral, Carboxamide, Chemical synthesis, Enzyme inhibitor, In vitro, Indole derivatives, Naphthalene derivatives, Non covalent bond, Peptidases, Protease inhibitor, Selectivity, Severe acute respiratory syndrome virus, Structure activity relation.

Abstract

A series of isatin derivatives were synthesized and tested against SARS CoV 3C-like protease. Substitutions at the N-1 and C-5 positions were examined to elucidate the differences in substrate binding sites of the rhinovirus 3C protease and SARS CoV 3C-like protease. Compound 5f shows significant inhibition with an IC₅₀ of 0.37 μM. Further study showed that, unlike the irreversible covalent binding of isatin derivatives to human rhinovirus 3C protease, the compounds tested in this study are all noncovalent reversible inhibitors.

Notice en format standard (ISO 2709)

Pour connaître la documentation sur le format Inist Standard.

A01	`01`	`1`		`@0 0022-2623`
A02	`01`			`@0 JMCMAR`
A03		`1`		`@0 J. med. chem. : (Print)`
A05				`@2 49`
A06				`@2 12`
A08	`01`	`1`	`ENG`	`@1 Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors`
A11	`01`	`1`		`@1 LU ZHOU`
A11	`02`	`1`		`@1 YING LIU`
A11	`03`	`1`		`@1 WEILIN ZHANG`
A11	`04`	`1`		`@1 PING WEI`
A11	`05`	`1`		`@1 CHANGKANG HUANG`
A11	`06`	`1`		`@1 JIANFENG PEI`
A11	`07`	`1`		`@1 YAXIA YUAN`
A11	`08`	`1`		`@1 LUHUA LAI`
A14	`01`			`@1 State Key Laboratory for Structural Chemistry of Unstable and Stable Species, College of Chemistry and Molecular Engineering, Peking University @2 Beijing 100871 @3 CHN @Z 1 aut. @Z 2 aut. @Z 3 aut. @Z 4 aut. @Z 5 aut. @Z 6 aut. @Z 7 aut. @Z 8 aut.`
A14	`02`			`@1 Center for Theoretical Biology, Peking University @2 Beijing 100871 @3 CHN @Z 6 aut. @Z 8 aut.`
A20				`@1 3440-3443`
A21				`@1 2006`
A23	`01`			`@0 ENG`
A43	`01`			`@1 INIST @2 9165 @5 354000156706810030`
A44				`@0 0000 @1 © 2006 INIST-CNRS. All rights reserved.`
A47	`01`	`1`		`@0 06-0478361`
A60				`@1 P @3 CR`
A61				`@0 A`
A64	`01`	`1`		`@0 Journal of medicinal chemistry : (Print)`
A66	`01`			`@0 USA`
A99				`@0 3/4 p. ref. et notes`
C01	`01`		`ENG`	@0 A series of isatin derivatives were synthesized and tested against SARS CoV 3C-like protease. Substitutions at the N-1 and C-5 positions were examined to elucidate the differences in substrate binding sites of the rhinovirus 3C protease and SARS CoV 3C-like protease. Compound 5f shows significant inhibition with an IC₅₀ of 0.37 μM. Further study showed that, unlike the irreversible covalent binding of isatin derivatives to human rhinovirus 3C protease, the compounds tested in this study are all noncovalent reversible inhibitors.
C02	`01`	`X`		`@0 002B02S05`
C03	`01`	`X`	`FRE`	`@0 Isatine @2 NK @2 FR @5 01`
C03	`02`	`X`	`FRE`	`@0 Virus syndrome respiratoire aigu sévère @2 NW @5 02`
C03	`02`	`X`	`ENG`	`@0 Severe acute respiratory syndrome virus @2 NW @5 02`
C03	`02`	`X`	`SPA`	`@0 Severe acute respiratory syndrome virus @2 NW @5 02`
C03	`03`	`X`	`FRE`	`@0 Inhibiteur protease @2 FR @5 03`
C03	`03`	`X`	`ENG`	`@0 Protease inhibitor @2 FR @5 03`
C03	`03`	`X`	`SPA`	`@0 Inhibidor proteasa @2 FR @5 03`
C03	`04`	`X`	`FRE`	`@0 Relation structure activité @5 04`
C03	`04`	`X`	`ENG`	`@0 Structure activity relation @5 04`
C03	`04`	`X`	`SPA`	`@0 Relación estructura actividad @5 04`
C03	`05`	`X`	`FRE`	`@0 In vitro @5 05`
C03	`05`	`X`	`ENG`	`@0 In vitro @5 05`
C03	`05`	`X`	`SPA`	`@0 In vitro @5 05`
C03	`06`	`X`	`FRE`	`@0 Sélectivité @5 06`
C03	`06`	`X`	`ENG`	`@0 Selectivity @5 06`
C03	`06`	`X`	`SPA`	`@0 Selectividad @5 06`
C03	`07`	`X`	`FRE`	`@0 Synthèse chimique @5 07`
C03	`07`	`X`	`ENG`	`@0 Chemical synthesis @5 07`
C03	`07`	`X`	`SPA`	`@0 Síntesis química @5 07`
C03	`08`	`X`	`FRE`	`@0 Naphtalène dérivé @5 08`
C03	`08`	`X`	`ENG`	`@0 Naphthalene derivatives @5 08`
C03	`08`	`X`	`SPA`	`@0 Naftaleno derivado @5 08`
C03	`09`	`X`	`FRE`	`@0 Carboxamide @5 09`
C03	`09`	`X`	`ENG`	`@0 Carboxamide @5 09`
C03	`09`	`X`	`SPA`	`@0 Carboxamida @5 09`
C03	`10`	`X`	`FRE`	`@0 Indole dérivé @5 32`
C03	`10`	`X`	`ENG`	`@0 Indole derivatives @5 32`
C03	`10`	`X`	`SPA`	`@0 Indol derivado @5 32`
C03	`11`	`X`	`FRE`	`@0 Peptidases @2 FE @5 33`
C03	`11`	`X`	`ENG`	`@0 Peptidases @2 FE @5 33`
C03	`11`	`X`	`SPA`	`@0 Peptidases @2 FE @5 33`
C03	`12`	`X`	`FRE`	`@0 Inhibiteur enzyme @5 34`
C03	`12`	`X`	`ENG`	`@0 Enzyme inhibitor @5 34`
C03	`12`	`X`	`SPA`	`@0 Inhibidor enzima @5 34`
C03	`13`	`X`	`FRE`	`@0 Antiviral @5 35`
C03	`13`	`X`	`ENG`	`@0 Antiviral @5 35`
C03	`13`	`X`	`SPA`	`@0 Antiviral @5 35`
C03	`14`	`X`	`FRE`	`@0 Indole-5-carboxamide(2,3-dihydro-2,3-dioxo-1-[2-naphtylméthyl]) @2 NK @4 INC @5 76`
C03	`15`	`X`	`FRE`	`@0 Liaison non covalente @4 CD @5 96`
C03	`15`	`X`	`ENG`	`@0 Non covalent bond @4 CD @5 96`
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				`@1 317`

Format Inist (serveur)

NO :	PASCAL 06-0478361 INIST
ET :	Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors
AU :	LU ZHOU; YING LIU; WEILIN ZHANG; PING WEI; CHANGKANG HUANG; JIANFENG PEI; YAXIA YUAN; LUHUA LAI
AF :	State Key Laboratory for Structural Chemistry of Unstable and Stable Species, College of Chemistry and Molecular Engineering, Peking University/Beijing 100871/Chine (1 aut., 2 aut., 3 aut., 4 aut., 5 aut., 6 aut., 7 aut., 8 aut.); Center for Theoretical Biology, Peking University/Beijing 100871/Chine (6 aut., 8 aut.)
DT :	Publication en série; Correspondance, lettre; Niveau analytique
SO :	Journal of medicinal chemistry : (Print); ISSN 0022-2623; Coden JMCMAR; Etats-Unis; Da. 2006; Vol. 49; No. 12; Pp. 3440-3443
LA :	Anglais
EA :	A series of isatin derivatives were synthesized and tested against SARS CoV 3C-like protease. Substitutions at the N-1 and C-5 positions were examined to elucidate the differences in substrate binding sites of the rhinovirus 3C protease and SARS CoV 3C-like protease. Compound 5f shows significant inhibition with an IC₅₀ of 0.37 μM. Further study showed that, unlike the irreversible covalent binding of isatin derivatives to human rhinovirus 3C protease, the compounds tested in this study are all noncovalent reversible inhibitors.
CC :	002B02S05
FD :	Isatine; Virus syndrome respiratoire aigu sévère; Inhibiteur protease; Relation structure activité; In vitro; Sélectivité; Synthèse chimique; Naphtalène dérivé; Carboxamide; Indole dérivé; Peptidases; Inhibiteur enzyme; Antiviral; Indole-5-carboxamide(2,3-dihydro-2,3-dioxo-1-[2-naphtylméth yl]); Liaison non covalente
FG :	Coronavirus; Coronaviridae; Nidovirales; Virus; Hydrolases; Enzyme
ED :	Severe acute respiratory syndrome virus; Protease inhibitor; Structure activity relation; In vitro; Selectivity; Chemical synthesis; Naphthalene derivatives; Carboxamide; Indole derivatives; Peptidases; Enzyme inhibitor; Antiviral; Non covalent bond
EG :	Coronavirus; Coronaviridae; Nidovirales; Virus; Hydrolases; Enzyme
SD :	Severe acute respiratory syndrome virus; Inhibidor proteasa; Relación estructura actividad; In vitro; Selectividad; Síntesis química; Naftaleno derivado; Carboxamida; Indol derivado; Peptidases; Inhibidor enzima; Antiviral
LO :	INIST-9165.354000156706810030
ID :	06-0478361

Links to Exploration step

Pascal:06-0478361

Le document en format XML

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<author><name sortKey="Changkang Huang" sort="Changkang Huang" uniqKey="Changkang Huang" last="Changkang Huang">CHANGKANG HUANG</name>
<affiliation><inist:fA14 i1="01"><s1>State Key Laboratory for Structural Chemistry of Unstable and Stable Species, College of Chemistry and Molecular Engineering, Peking University</s1>
<s2>Beijing 100871</s2>
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<author><name sortKey="Jianfeng Pei" sort="Jianfeng Pei" uniqKey="Jianfeng Pei" last="Jianfeng Pei">JIANFENG PEI</name>
<affiliation><inist:fA14 i1="01"><s1>State Key Laboratory for Structural Chemistry of Unstable and Stable Species, College of Chemistry and Molecular Engineering, Peking University</s1>
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<author><name sortKey="Yaxia Yuan" sort="Yaxia Yuan" uniqKey="Yaxia Yuan" last="Yaxia Yuan">YAXIA YUAN</name>
<affiliation><inist:fA14 i1="01"><s1>State Key Laboratory for Structural Chemistry of Unstable and Stable Species, College of Chemistry and Molecular Engineering, Peking University</s1>
<s2>Beijing 100871</s2>
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<author><name sortKey="Luhua Lai" sort="Luhua Lai" uniqKey="Luhua Lai" last="Luhua Lai">LUHUA LAI</name>
<affiliation><inist:fA14 i1="01"><s1>State Key Laboratory for Structural Chemistry of Unstable and Stable Species, College of Chemistry and Molecular Engineering, Peking University</s1>
<s2>Beijing 100871</s2>
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<affiliation><inist:fA14 i1="02"><s1>Center for Theoretical Biology, Peking University</s1>
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<series><title level="j" type="main">Journal of medicinal chemistry : (Print)</title>
<title level="j" type="abbreviated">J. med. chem. : (Print)</title>
<idno type="ISSN">0022-2623</idno>
<imprint><date when="2006">2006</date>
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<term>Carboxamide</term>
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<term>Enzyme inhibitor</term>
<term>In vitro</term>
<term>Indole derivatives</term>
<term>Naphthalene derivatives</term>
<term>Non covalent bond</term>
<term>Peptidases</term>
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<term>Selectivity</term>
<term>Severe acute respiratory syndrome virus</term>
<term>Structure activity relation</term>
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<keywords scheme="Pascal" xml:lang="fr"><term>Isatine</term>
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<term>Synthèse chimique</term>
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<term>Antiviral</term>
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<front><div type="abstract" xml:lang="en">A series of isatin derivatives were synthesized and tested against SARS CoV 3C-like protease. Substitutions at the N-1 and C-5 positions were examined to elucidate the differences in substrate binding sites of the rhinovirus 3C protease and SARS CoV 3C-like protease. Compound 5f shows significant inhibition with an IC<sub>50</sub>
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<fA08 i1="01" i2="1" l="ENG"><s1>Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors</s1>
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<fA11 i1="01" i2="1"><s1>LU ZHOU</s1>
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<fA11 i1="02" i2="1"><s1>YING LIU</s1>
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<fA11 i1="03" i2="1"><s1>WEILIN ZHANG</s1>
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<fA11 i1="04" i2="1"><s1>PING WEI</s1>
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<fA11 i1="07" i2="1"><s1>YAXIA YUAN</s1>
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<fA14 i1="01"><s1>State Key Laboratory for Structural Chemistry of Unstable and Stable Species, College of Chemistry and Molecular Engineering, Peking University</s1>
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<s3>CHN</s3>
<sZ>1 aut.</sZ>
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<sZ>3 aut.</sZ>
<sZ>4 aut.</sZ>
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<sZ>7 aut.</sZ>
<sZ>8 aut.</sZ>
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<fC01 i1="01" l="ENG"><s0>A series of isatin derivatives were synthesized and tested against SARS CoV 3C-like protease. Substitutions at the N-1 and C-5 positions were examined to elucidate the differences in substrate binding sites of the rhinovirus 3C protease and SARS CoV 3C-like protease. Compound 5f shows significant inhibition with an IC<sub>50</sub>
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<server><NO>PASCAL 06-0478361 INIST</NO>
<ET>Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors</ET>
<AU>LU ZHOU; YING LIU; WEILIN ZHANG; PING WEI; CHANGKANG HUANG; JIANFENG PEI; YAXIA YUAN; LUHUA LAI</AU>
<AF>State Key Laboratory for Structural Chemistry of Unstable and Stable Species, College of Chemistry and Molecular Engineering, Peking University/Beijing 100871/Chine (1 aut., 2 aut., 3 aut., 4 aut., 5 aut., 6 aut., 7 aut., 8 aut.); Center for Theoretical Biology, Peking University/Beijing 100871/Chine (6 aut., 8 aut.)</AF>
<DT>Publication en série; Correspondance, lettre; Niveau analytique</DT>
<SO>Journal of medicinal chemistry : (Print); ISSN 0022-2623; Coden JMCMAR; Etats-Unis; Da. 2006; Vol. 49; No. 12; Pp. 3440-3443</SO>
<LA>Anglais</LA>
<EA>A series of isatin derivatives were synthesized and tested against SARS CoV 3C-like protease. Substitutions at the N-1 and C-5 positions were examined to elucidate the differences in substrate binding sites of the rhinovirus 3C protease and SARS CoV 3C-like protease. Compound 5f shows significant inhibition with an IC<sub>50</sub>
 of 0.37 μM. Further study showed that, unlike the irreversible covalent binding of isatin derivatives to human rhinovirus 3C protease, the compounds tested in this study are all noncovalent reversible inhibitors.</EA>
<CC>002B02S05</CC>
<FD>Isatine; Virus syndrome respiratoire aigu sévère; Inhibiteur protease; Relation structure activité; In vitro; Sélectivité; Synthèse chimique; Naphtalène dérivé; Carboxamide; Indole dérivé; Peptidases; Inhibiteur enzyme; Antiviral; Indole-5-carboxamide(2,3-dihydro-2,3-dioxo-1-[2-naphtylméth yl]); Liaison non covalente</FD>
<FG>Coronavirus; Coronaviridae; Nidovirales; Virus; Hydrolases; Enzyme</FG>
<ED>Severe acute respiratory syndrome virus; Protease inhibitor; Structure activity relation; In vitro; Selectivity; Chemical synthesis; Naphthalene derivatives; Carboxamide; Indole derivatives; Peptidases; Enzyme inhibitor; Antiviral; Non covalent bond</ED>
<EG>Coronavirus; Coronaviridae; Nidovirales; Virus; Hydrolases; Enzyme</EG>
<SD>Severe acute respiratory syndrome virus; Inhibidor proteasa; Relación estructura actividad; In vitro; Selectividad; Síntesis química; Naftaleno derivado; Carboxamida; Indol derivado; Peptidases; Inhibidor enzima; Antiviral</SD>
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Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors

Isatin compounds as noncovalent SARS coronavirus 3C-like protease inhibitors

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