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Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity

Identifieur interne : 000515 ( PascalFrancis/Corpus ); précédent : 000514; suivant : 000516

Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity

Auteurs : Caterina Fattorusso ; Sandra Gemma ; Stefania Butini ; Paul Huleatt ; Bruno Catalanotti ; Marco Persico ; Meri De Angelis ; Isabella Fiorini ; V Ito Nacci ; Anna Ramunno ; Manuela Rodriquez ; Giovanni Greco ; Ettore Novellino ; Alberto Bergamini ; Stefano Marini ; Massimo Coletta ; Giovanni Maga ; Silvio Spadari ; Giuseppe Campiani

Source :

RBID : Pascal:06-0200728

Descripteurs français

English descriptors

Abstract

Pyrrolobenzoxazepinones (PBOs) represent a new class of human immunodeficiency virus type 1 (HIV-1) nonnucleoside reverse transcriptase (RT) inhibitors (NNRTIs) whose prototype is 5. Molecular modeling studies based on the X-ray structures of HIV-1 RT prompted the synthesis of novel analogues which were tested as anti-HIV agents. The PBO derivatives specifically designed to target the highly conserved amino acid residues within the β12-β13 hairpin, namely primer grip, proved to be very potent against the most common mutant enzymes, including the highly resistant K103N mutant strain. Structure-activity relationships (SARs) are discussed in terms of a possible interaction with the RT binding site, depending on the nature of the substituents at C-6. Among the pyrrolobenzoxazepines investigated, 15c appeared to be the most promising NNRTI of the series characterized by potent antiviral activity, broad spectrum, and low cytotoxicity. 15c showed synergistic antiviral activity with AZT.

Notice en format standard (ISO 2709)

Pour connaître la documentation sur le format Inist Standard.

pA  
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A02 01      @0 JMCMAR
A03   1    @0 J. med. chem. : (Print)
A05       @2 48
A06       @2 23
A08 01  1  ENG  @1 Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity
A11 01  1    @1 FATTORUSSO (Caterina)
A11 02  1    @1 GEMMA (Sandra)
A11 03  1    @1 BUTINI (Stefania)
A11 04  1    @1 HULEATT (Paul)
A11 05  1    @1 CATALANOTTI (Bruno)
A11 06  1    @1 PERSICO (Marco)
A11 07  1    @1 DE ANGELIS (Meri)
A11 08  1    @1 FIORINI (Isabella)
A11 09  1    @1 NACCI (V Ito)
A11 10  1    @1 RAMUNNO (Anna)
A11 11  1    @1 RODRIQUEZ (Manuela)
A11 12  1    @1 GRECO (Giovanni)
A11 13  1    @1 NOVELLINO (Ettore)
A11 14  1    @1 BERGAMINI (Alberto)
A11 15  1    @1 MARINI (Stefano)
A11 16  1    @1 COLETTA (Massimo)
A11 17  1    @1 MAGA (Giovanni)
A11 18  1    @1 SPADARI (Silvio)
A11 19  1    @1 CAMPIANI (Giuseppe)
A14 01      @1 Dipartimento Farmaco Chimico Tecnologico, via Aldo Moro, European Research Centre for Drug Discovery and Development, Universita' degli Studi di Siena @2 53100 Siena @3 ITA @Z 1 aut. @Z 2 aut. @Z 3 aut. @Z 4 aut. @Z 5 aut. @Z 6 aut. @Z 7 aut. @Z 8 aut. @Z 9 aut. @Z 12 aut. @Z 13 aut. @Z 18 aut. @Z 19 aut.
A14 02      @1 Dipartimento di Chimica delle Sostanze Naturali e Dipartimento di Chimica Farmaceutica e Tossicologica, Universita' di Napoli "Federico II", via D. Montesano 49 @2 80131 Napoli @3 ITA @Z 2 aut. @Z 3 aut. @Z 4 aut. @Z 7 aut. @Z 8 aut. @Z 9 aut. @Z 10 aut. @Z 11 aut. @Z 19 aut.
A14 03      @1 Dipartimento di Sanita' Pubblica e Biologia Cellulare (DSP&BC), Universita' degli Studi di Roma "Tor Vergata", via Tor Vergata 135 @2 00133 Roma @3 ITA @Z 5 aut.
A14 04      @1 Dipartimento di Medicina Sperimentale e Scienze Biochimiche (DMS&SB), Universita' degli Studi di Roma Tor Vergata, via Tor Vergata 135 @2 00133 Roma @3 ITA @Z 14 aut. @Z 15 aut. @Z 16 aut.
A14 05      @1 Istituto di Genetica Molecolare (IGM) - CNR, via Abbiategrasso 207 @2 27100 Pavia @3 ITA @Z 17 aut. @Z 18 aut.
A20       @1 7153-7165
A21       @1 2005
A23 01      @0 ENG
A43 01      @1 INIST @2 9165 @5 354000135190880100
A44       @0 0000 @1 © 2006 INIST-CNRS. All rights reserved.
A47 01  1    @0 06-0200728
A60       @1 P
A61       @0 A
A64 01  1    @0 Journal of medicinal chemistry : (Print)
A66 01      @0 USA
A99       @0 1 p.1/2 ref. et notes
C01 01    ENG  @0 Pyrrolobenzoxazepinones (PBOs) represent a new class of human immunodeficiency virus type 1 (HIV-1) nonnucleoside reverse transcriptase (RT) inhibitors (NNRTIs) whose prototype is 5. Molecular modeling studies based on the X-ray structures of HIV-1 RT prompted the synthesis of novel analogues which were tested as anti-HIV agents. The PBO derivatives specifically designed to target the highly conserved amino acid residues within the β12-β13 hairpin, namely primer grip, proved to be very potent against the most common mutant enzymes, including the highly resistant K103N mutant strain. Structure-activity relationships (SARs) are discussed in terms of a possible interaction with the RT binding site, depending on the nature of the substituents at C-6. Among the pyrrolobenzoxazepines investigated, 15c appeared to be the most promising NNRTI of the series characterized by potent antiviral activity, broad spectrum, and low cytotoxicity. 15c showed synergistic antiviral activity with AZT.
C02 01  X    @0 002B02S05
C03 01  X  FRE  @0 Ciblage @5 01
C03 01  X  ENG  @0 Targeting @5 01
C03 01  X  SPA  @0 Blancado @5 01
C03 02  X  FRE  @0 Virus HIV1 @2 NW @5 02
C03 02  X  ENG  @0 HIV-1 virus @2 NW @5 02
C03 02  X  SPA  @0 HIV-1 virus @2 NW @5 02
C03 03  X  FRE  @0 RNA-directed DNA polymerase @2 FE @5 03
C03 03  X  ENG  @0 RNA-directed DNA polymerase @2 FE @5 03
C03 03  X  SPA  @0 RNA-directed DNA polymerase @2 FE @5 03
C03 04  X  FRE  @0 Synthèse chimique @5 04
C03 04  X  ENG  @0 Chemical synthesis @5 04
C03 04  X  SPA  @0 Síntesis química @5 04
C03 05  X  FRE  @0 Relation structure activité @5 05
C03 05  X  ENG  @0 Structure activity relation @5 05
C03 05  X  SPA  @0 Relación estructura actividad @5 05
C03 06  X  FRE  @0 Inhibiteur reverse transcriptase @2 NK @2 FR @5 06
C03 06  X  ENG  @0 Reverse transcriptase inhibitor @2 NK @2 FR @5 06
C03 06  X  SPA  @0 Inhibitor reverse transcriptase @2 NK @2 FR @5 06
C03 07  X  FRE  @0 Composé non nucléoside @5 07
C03 07  X  ENG  @0 Non nucleoside compound @5 07
C03 07  X  SPA  @0 Compuesto no nucleósido @5 07
C03 08  X  FRE  @0 Antiviral @5 08
C03 08  X  ENG  @0 Antiviral @5 08
C03 08  X  SPA  @0 Antiviral @5 08
C03 09  X  FRE  @0 In vitro @5 09
C03 09  X  ENG  @0 In vitro @5 09
C03 09  X  SPA  @0 In vitro @5 09
C03 10  X  FRE  @0 Association médicamenteuse @5 10
C03 10  X  ENG  @0 Drug combination @5 10
C03 10  X  SPA  @0 Asociación medicamentosa @5 10
C03 11  X  FRE  @0 Interaction médicamenteuse @5 11
C03 11  X  ENG  @0 Drug interaction @5 11
C03 11  X  SPA  @0 Interacción medicamentosa @5 11
C03 12  X  FRE  @0 Synergie @5 12
C03 12  X  ENG  @0 Synergism @5 12
C03 12  X  SPA  @0 Sinergia @5 12
C03 13  X  FRE  @0 Zidovudine @2 NK @2 FR @5 13
C03 13  X  ENG  @0 Zidovudine @2 NK @2 FR @5 13
C03 13  X  SPA  @0 Zidovudina @2 NK @2 FR @5 13
C03 14  X  FRE  @0 Inhibiteur enzyme @5 32
C03 14  X  ENG  @0 Enzyme inhibitor @5 32
C03 14  X  SPA  @0 Inhibidor enzima @5 32
C03 15  X  FRE  @0 Pyrrolobenzooxazépine @4 INC @5 76
C03 16  X  FRE  @0 Pyrrolo[2,1-d][1,5]benzooxazépin-7-one(6-éthyl-6-[4-(phénoxyméthyl)phényl]) @2 NK @4 INC @5 77
C03 17  X  FRE  @0 Lignée C8166 @4 INC @5 78
C07 01  X  FRE  @0 Virus immunodéficience humaine @2 NW
C07 01  X  ENG  @0 Human immunodeficiency virus @2 NW
C07 01  X  SPA  @0 Human immunodeficiency virus @2 NW
C07 02  X  FRE  @0 Lentivirus @2 NW
C07 02  X  ENG  @0 Lentivirus @2 NW
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C07 03  X  ENG  @0 Retroviridae @2 NW
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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 Nucleotidyltransferases @2 FE
C07 05  X  ENG  @0 Nucleotidyltransferases @2 FE
C07 05  X  SPA  @0 Nucleotidyltransferases @2 FE
C07 06  X  FRE  @0 Transferases @2 FE
C07 06  X  ENG  @0 Transferases @2 FE
C07 06  X  SPA  @0 Transferases @2 FE
C07 07  X  FRE  @0 Enzyme @2 FE
C07 07  X  ENG  @0 Enzyme @2 FE
C07 07  X  SPA  @0 Enzima @2 FE
N21       @1 128

Format Inist (serveur)

NO : PASCAL 06-0200728 INIST
ET : Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity
AU : FATTORUSSO (Caterina); GEMMA (Sandra); BUTINI (Stefania); HULEATT (Paul); CATALANOTTI (Bruno); PERSICO (Marco); DE ANGELIS (Meri); FIORINI (Isabella); NACCI (V Ito); RAMUNNO (Anna); RODRIQUEZ (Manuela); GRECO (Giovanni); NOVELLINO (Ettore); BERGAMINI (Alberto); MARINI (Stefano); COLETTA (Massimo); MAGA (Giovanni); SPADARI (Silvio); CAMPIANI (Giuseppe)
AF : Dipartimento Farmaco Chimico Tecnologico, via Aldo Moro, European Research Centre for Drug Discovery and Development, Universita' degli Studi di Siena/53100 Siena/Italie (1 aut., 2 aut., 3 aut., 4 aut., 5 aut., 6 aut., 7 aut., 8 aut., 9 aut., 12 aut., 13 aut., 18 aut., 19 aut.); Dipartimento di Chimica delle Sostanze Naturali e Dipartimento di Chimica Farmaceutica e Tossicologica, Universita' di Napoli "Federico II", via D. Montesano 49/80131 Napoli/Italie (2 aut., 3 aut., 4 aut., 7 aut., 8 aut., 9 aut., 10 aut., 11 aut., 19 aut.); Dipartimento di Sanita' Pubblica e Biologia Cellulare (DSP&BC), Universita' degli Studi di Roma "Tor Vergata", via Tor Vergata 135/00133 Roma/Italie (5 aut.); Dipartimento di Medicina Sperimentale e Scienze Biochimiche (DMS&SB), Universita' degli Studi di Roma Tor Vergata, via Tor Vergata 135/00133 Roma/Italie (14 aut., 15 aut., 16 aut.); Istituto di Genetica Molecolare (IGM) - CNR, via Abbiategrasso 207/27100 Pavia/Italie (17 aut., 18 aut.)
DT : Publication en série; Niveau analytique
SO : Journal of medicinal chemistry : (Print); ISSN 0022-2623; Coden JMCMAR; Etats-Unis; Da. 2005; Vol. 48; No. 23; Pp. 7153-7165
LA : Anglais
EA : Pyrrolobenzoxazepinones (PBOs) represent a new class of human immunodeficiency virus type 1 (HIV-1) nonnucleoside reverse transcriptase (RT) inhibitors (NNRTIs) whose prototype is 5. Molecular modeling studies based on the X-ray structures of HIV-1 RT prompted the synthesis of novel analogues which were tested as anti-HIV agents. The PBO derivatives specifically designed to target the highly conserved amino acid residues within the β12-β13 hairpin, namely primer grip, proved to be very potent against the most common mutant enzymes, including the highly resistant K103N mutant strain. Structure-activity relationships (SARs) are discussed in terms of a possible interaction with the RT binding site, depending on the nature of the substituents at C-6. Among the pyrrolobenzoxazepines investigated, 15c appeared to be the most promising NNRTI of the series characterized by potent antiviral activity, broad spectrum, and low cytotoxicity. 15c showed synergistic antiviral activity with AZT.
CC : 002B02S05
FD : Ciblage; Virus HIV1; RNA-directed DNA polymerase; Synthèse chimique; Relation structure activité; Inhibiteur reverse transcriptase; Composé non nucléoside; Antiviral; In vitro; Association médicamenteuse; Interaction médicamenteuse; Synergie; Zidovudine; Inhibiteur enzyme; Pyrrolobenzooxazépine; Pyrrolo[2,1-d][1,5]be nzooxazépin-7-one(6-éthyl-6-[4-(phénoxyméthyl)phényl]); Lignée C8166
FG : Virus immunodéficience humaine; Lentivirus; Retroviridae; Virus; Nucleotidyltransferases; Transferases; Enzyme
ED : Targeting; HIV-1 virus; RNA-directed DNA polymerase; Chemical synthesis; Structure activity relation; Reverse transcriptase inhibitor; Non nucleoside compound; Antiviral; In vitro; Drug combination; Drug interaction; Synergism; Zidovudine; Enzyme inhibitor
EG : Human immunodeficiency virus; Lentivirus; Retroviridae; Virus; Nucleotidyltransferases; Transferases; Enzyme
SD : Blancado; HIV-1 virus; RNA-directed DNA polymerase; Síntesis química; Relación estructura actividad; Inhibitor reverse transcriptase; Compuesto no nucleósido; Antiviral; In vitro; Asociación medicamentosa; Interacción medicamentosa; Sinergia; Zidovudina; Inhibidor enzima
LO : INIST-9165.354000135190880100
ID : 06-0200728

Links to Exploration step

Pascal:06-0200728

Le document en format XML

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<term>Antiviral</term>
<term>Chemical synthesis</term>
<term>Drug combination</term>
<term>Drug interaction</term>
<term>Enzyme inhibitor</term>
<term>HIV-1 virus</term>
<term>In vitro</term>
<term>Non nucleoside compound</term>
<term>RNA-directed DNA polymerase</term>
<term>Reverse transcriptase inhibitor</term>
<term>Structure activity relation</term>
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<term>Ciblage</term>
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<term>Pyrrolobenzooxazépine</term>
<term>Pyrrolo[2,1-d][1,5]benzooxazépin-7-one(6-éthyl-6-[4-(phénoxyméthyl)phényl])</term>
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<div type="abstract" xml:lang="en">Pyrrolobenzoxazepinones (PBOs) represent a new class of human immunodeficiency virus type 1 (HIV-1) nonnucleoside reverse transcriptase (RT) inhibitors (NNRTIs) whose prototype is 5. Molecular modeling studies based on the X-ray structures of HIV-1 RT prompted the synthesis of novel analogues which were tested as anti-HIV agents. The PBO derivatives specifically designed to target the highly conserved amino acid residues within the β12-β13 hairpin, namely primer grip, proved to be very potent against the most common mutant enzymes, including the highly resistant K103N mutant strain. Structure-activity relationships (SARs) are discussed in terms of a possible interaction with the RT binding site, depending on the nature of the substituents at C-6. Among the pyrrolobenzoxazepines investigated, 15c appeared to be the most promising NNRTI of the series characterized by potent antiviral activity, broad spectrum, and low cytotoxicity. 15c showed synergistic antiviral activity with AZT.</div>
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<s0>Inhibiteur reverse transcriptase</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>06</s5>
</fC03>
<fC03 i1="06" i2="X" l="ENG">
<s0>Reverse transcriptase inhibitor</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>06</s5>
</fC03>
<fC03 i1="06" i2="X" l="SPA">
<s0>Inhibitor reverse transcriptase</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>06</s5>
</fC03>
<fC03 i1="07" i2="X" l="FRE">
<s0>Composé non nucléoside</s0>
<s5>07</s5>
</fC03>
<fC03 i1="07" i2="X" l="ENG">
<s0>Non nucleoside compound</s0>
<s5>07</s5>
</fC03>
<fC03 i1="07" i2="X" l="SPA">
<s0>Compuesto no nucleósido</s0>
<s5>07</s5>
</fC03>
<fC03 i1="08" i2="X" l="FRE">
<s0>Antiviral</s0>
<s5>08</s5>
</fC03>
<fC03 i1="08" i2="X" l="ENG">
<s0>Antiviral</s0>
<s5>08</s5>
</fC03>
<fC03 i1="08" i2="X" l="SPA">
<s0>Antiviral</s0>
<s5>08</s5>
</fC03>
<fC03 i1="09" i2="X" l="FRE">
<s0>In vitro</s0>
<s5>09</s5>
</fC03>
<fC03 i1="09" i2="X" l="ENG">
<s0>In vitro</s0>
<s5>09</s5>
</fC03>
<fC03 i1="09" i2="X" l="SPA">
<s0>In vitro</s0>
<s5>09</s5>
</fC03>
<fC03 i1="10" i2="X" l="FRE">
<s0>Association médicamenteuse</s0>
<s5>10</s5>
</fC03>
<fC03 i1="10" i2="X" l="ENG">
<s0>Drug combination</s0>
<s5>10</s5>
</fC03>
<fC03 i1="10" i2="X" l="SPA">
<s0>Asociación medicamentosa</s0>
<s5>10</s5>
</fC03>
<fC03 i1="11" i2="X" l="FRE">
<s0>Interaction médicamenteuse</s0>
<s5>11</s5>
</fC03>
<fC03 i1="11" i2="X" l="ENG">
<s0>Drug interaction</s0>
<s5>11</s5>
</fC03>
<fC03 i1="11" i2="X" l="SPA">
<s0>Interacción medicamentosa</s0>
<s5>11</s5>
</fC03>
<fC03 i1="12" i2="X" l="FRE">
<s0>Synergie</s0>
<s5>12</s5>
</fC03>
<fC03 i1="12" i2="X" l="ENG">
<s0>Synergism</s0>
<s5>12</s5>
</fC03>
<fC03 i1="12" i2="X" l="SPA">
<s0>Sinergia</s0>
<s5>12</s5>
</fC03>
<fC03 i1="13" i2="X" l="FRE">
<s0>Zidovudine</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>13</s5>
</fC03>
<fC03 i1="13" i2="X" l="ENG">
<s0>Zidovudine</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>13</s5>
</fC03>
<fC03 i1="13" i2="X" l="SPA">
<s0>Zidovudina</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>13</s5>
</fC03>
<fC03 i1="14" i2="X" l="FRE">
<s0>Inhibiteur enzyme</s0>
<s5>32</s5>
</fC03>
<fC03 i1="14" i2="X" l="ENG">
<s0>Enzyme inhibitor</s0>
<s5>32</s5>
</fC03>
<fC03 i1="14" i2="X" l="SPA">
<s0>Inhibidor enzima</s0>
<s5>32</s5>
</fC03>
<fC03 i1="15" i2="X" l="FRE">
<s0>Pyrrolobenzooxazépine</s0>
<s4>INC</s4>
<s5>76</s5>
</fC03>
<fC03 i1="16" i2="X" l="FRE">
<s0>Pyrrolo[2,1-d][1,5]benzooxazépin-7-one(6-éthyl-6-[4-(phénoxyméthyl)phényl])</s0>
<s2>NK</s2>
<s4>INC</s4>
<s5>77</s5>
</fC03>
<fC03 i1="17" i2="X" l="FRE">
<s0>Lignée C8166</s0>
<s4>INC</s4>
<s5>78</s5>
</fC03>
<fC07 i1="01" i2="X" l="FRE">
<s0>Virus immunodéficience humaine</s0>
<s2>NW</s2>
</fC07>
<fC07 i1="01" i2="X" l="ENG">
<s0>Human immunodeficiency virus</s0>
<s2>NW</s2>
</fC07>
<fC07 i1="01" i2="X" l="SPA">
<s0>Human immunodeficiency virus</s0>
<s2>NW</s2>
</fC07>
<fC07 i1="02" i2="X" l="FRE">
<s0>Lentivirus</s0>
<s2>NW</s2>
</fC07>
<fC07 i1="02" i2="X" l="ENG">
<s0>Lentivirus</s0>
<s2>NW</s2>
</fC07>
<fC07 i1="02" i2="X" l="SPA">
<s0>Lentivirus</s0>
<s2>NW</s2>
</fC07>
<fC07 i1="03" i2="X" l="FRE">
<s0>Retroviridae</s0>
<s2>NW</s2>
</fC07>
<fC07 i1="03" i2="X" l="ENG">
<s0>Retroviridae</s0>
<s2>NW</s2>
</fC07>
<fC07 i1="03" i2="X" l="SPA">
<s0>Retroviridae</s0>
<s2>NW</s2>
</fC07>
<fC07 i1="04" i2="X" l="FRE">
<s0>Virus</s0>
<s2>NW</s2>
</fC07>
<fC07 i1="04" i2="X" l="ENG">
<s0>Virus</s0>
<s2>NW</s2>
</fC07>
<fC07 i1="04" i2="X" l="SPA">
<s0>Virus</s0>
<s2>NW</s2>
</fC07>
<fC07 i1="05" i2="X" l="FRE">
<s0>Nucleotidyltransferases</s0>
<s2>FE</s2>
</fC07>
<fC07 i1="05" i2="X" l="ENG">
<s0>Nucleotidyltransferases</s0>
<s2>FE</s2>
</fC07>
<fC07 i1="05" i2="X" l="SPA">
<s0>Nucleotidyltransferases</s0>
<s2>FE</s2>
</fC07>
<fC07 i1="06" i2="X" l="FRE">
<s0>Transferases</s0>
<s2>FE</s2>
</fC07>
<fC07 i1="06" i2="X" l="ENG">
<s0>Transferases</s0>
<s2>FE</s2>
</fC07>
<fC07 i1="06" i2="X" l="SPA">
<s0>Transferases</s0>
<s2>FE</s2>
</fC07>
<fC07 i1="07" i2="X" l="FRE">
<s0>Enzyme</s0>
<s2>FE</s2>
</fC07>
<fC07 i1="07" i2="X" l="ENG">
<s0>Enzyme</s0>
<s2>FE</s2>
</fC07>
<fC07 i1="07" i2="X" l="SPA">
<s0>Enzima</s0>
<s2>FE</s2>
</fC07>
<fN21>
<s1>128</s1>
</fN21>
</pA>
</standard>
<server>
<NO>PASCAL 06-0200728 INIST</NO>
<ET>Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity</ET>
<AU>FATTORUSSO (Caterina); GEMMA (Sandra); BUTINI (Stefania); HULEATT (Paul); CATALANOTTI (Bruno); PERSICO (Marco); DE ANGELIS (Meri); FIORINI (Isabella); NACCI (V Ito); RAMUNNO (Anna); RODRIQUEZ (Manuela); GRECO (Giovanni); NOVELLINO (Ettore); BERGAMINI (Alberto); MARINI (Stefano); COLETTA (Massimo); MAGA (Giovanni); SPADARI (Silvio); CAMPIANI (Giuseppe)</AU>
<AF>Dipartimento Farmaco Chimico Tecnologico, via Aldo Moro, European Research Centre for Drug Discovery and Development, Universita' degli Studi di Siena/53100 Siena/Italie (1 aut., 2 aut., 3 aut., 4 aut., 5 aut., 6 aut., 7 aut., 8 aut., 9 aut., 12 aut., 13 aut., 18 aut., 19 aut.); Dipartimento di Chimica delle Sostanze Naturali e Dipartimento di Chimica Farmaceutica e Tossicologica, Universita' di Napoli "Federico II", via D. Montesano 49/80131 Napoli/Italie (2 aut., 3 aut., 4 aut., 7 aut., 8 aut., 9 aut., 10 aut., 11 aut., 19 aut.); Dipartimento di Sanita' Pubblica e Biologia Cellulare (DSP&BC), Universita' degli Studi di Roma "Tor Vergata", via Tor Vergata 135/00133 Roma/Italie (5 aut.); Dipartimento di Medicina Sperimentale e Scienze Biochimiche (DMS&SB), Universita' degli Studi di Roma Tor Vergata, via Tor Vergata 135/00133 Roma/Italie (14 aut., 15 aut., 16 aut.); Istituto di Genetica Molecolare (IGM) - CNR, via Abbiategrasso 207/27100 Pavia/Italie (17 aut., 18 aut.)</AF>
<DT>Publication en série; Niveau analytique</DT>
<SO>Journal of medicinal chemistry : (Print); ISSN 0022-2623; Coden JMCMAR; Etats-Unis; Da. 2005; Vol. 48; No. 23; Pp. 7153-7165</SO>
<LA>Anglais</LA>
<EA>Pyrrolobenzoxazepinones (PBOs) represent a new class of human immunodeficiency virus type 1 (HIV-1) nonnucleoside reverse transcriptase (RT) inhibitors (NNRTIs) whose prototype is 5. Molecular modeling studies based on the X-ray structures of HIV-1 RT prompted the synthesis of novel analogues which were tested as anti-HIV agents. The PBO derivatives specifically designed to target the highly conserved amino acid residues within the β12-β13 hairpin, namely primer grip, proved to be very potent against the most common mutant enzymes, including the highly resistant K103N mutant strain. Structure-activity relationships (SARs) are discussed in terms of a possible interaction with the RT binding site, depending on the nature of the substituents at C-6. Among the pyrrolobenzoxazepines investigated, 15c appeared to be the most promising NNRTI of the series characterized by potent antiviral activity, broad spectrum, and low cytotoxicity. 15c showed synergistic antiviral activity with AZT.</EA>
<CC>002B02S05</CC>
<FD>Ciblage; Virus HIV1; RNA-directed DNA polymerase; Synthèse chimique; Relation structure activité; Inhibiteur reverse transcriptase; Composé non nucléoside; Antiviral; In vitro; Association médicamenteuse; Interaction médicamenteuse; Synergie; Zidovudine; Inhibiteur enzyme; Pyrrolobenzooxazépine; Pyrrolo[2,1-d][1,5]be nzooxazépin-7-one(6-éthyl-6-[4-(phénoxyméthyl)phényl]); Lignée C8166</FD>
<FG>Virus immunodéficience humaine; Lentivirus; Retroviridae; Virus; Nucleotidyltransferases; Transferases; Enzyme</FG>
<ED>Targeting; HIV-1 virus; RNA-directed DNA polymerase; Chemical synthesis; Structure activity relation; Reverse transcriptase inhibitor; Non nucleoside compound; Antiviral; In vitro; Drug combination; Drug interaction; Synergism; Zidovudine; Enzyme inhibitor</ED>
<EG>Human immunodeficiency virus; Lentivirus; Retroviridae; Virus; Nucleotidyltransferases; Transferases; Enzyme</EG>
<SD>Blancado; HIV-1 virus; RNA-directed DNA polymerase; Síntesis química; Relación estructura actividad; Inhibitor reverse transcriptase; Compuesto no nucleósido; Antiviral; In vitro; Asociación medicamentosa; Interacción medicamentosa; Sinergia; Zidovudina; Inhibidor enzima</SD>
<LO>INIST-9165.354000135190880100</LO>
<ID>06-0200728</ID>
</server>
</inist>
</record>

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