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Mariajose Camarasa - One of the best experts on this subject based on the ideXlab platform.

  • tsao analogues stereospecific synthesis and anti hiv 1 activity of 1 2 5 bis o tert butyldimethylsilyl beta d ribofuranosyl 3 spiro 5 4 amino 1 2 oxathiole 2 2 dioxide pyrimidine and pyrimidine modified nucleosides
    Journal of Medicinal Chemistry, 1992
    Co-Authors: Mariajesus Perezperez, Ana Sanfelix, Jan Balzarini, Erik De Clercq, Mariajose Camarasa
    Abstract:

    Several analogues of a new lead for anti-HIV-1 agents [1-[2',5'-bis-O-(Tert-Butyldimethylsilyl)-beta-D-ribofuranosyl]-thymine] -3'-spiro-5''-(4''-amino-1'',2''-oxathiole 2'',2''-dioxide) (TSAO) modified at positions N-3, O-4 and C-5 of the thymine moiety, have been prepared and evaluated as inhibitors of HIV-1 replication. A new stereoselective synthetic procedure is described. Reaction of 1,2-di-O-acetyl-5-O-benzoyl-3-C-cyano-3-O-mesyl-D-ribofuranose with pyrimidine bases, followed by treatment with Cs2CO3 afforded stereoselectively, beta-D-ribofuranosyl-3'-spiro nucleosides. 2',5'-O-Deacylation and subsequent treatment with Tert-Butyldimethylsilyl Chloride gave the TSAO derivatives. Only those analogues having a tBDMSi group at both the C-5' and C-2' positions of the ribose moiety showed potent anti-HIV-1 activity. The activity ranged from 0.060 microM to 1.0 microM. Introduction of an alkyl or alkenyl function at N-3 of the thymine ring markedly decreased cytotoxicity without affecting the antiviral activity. While markedly active against HIV-1, the TSAO derivatives had no activity against HIV-2 or SIV. They represent the first example of nucleoside analogues with an intact ribose moiety that discriminate between HIV-1 and other retroviruses.

Mariajesus Perezperez - One of the best experts on this subject based on the ideXlab platform.

  • tsao analogues stereospecific synthesis and anti hiv 1 activity of 1 2 5 bis o tert butyldimethylsilyl beta d ribofuranosyl 3 spiro 5 4 amino 1 2 oxathiole 2 2 dioxide pyrimidine and pyrimidine modified nucleosides
    Journal of Medicinal Chemistry, 1992
    Co-Authors: Mariajesus Perezperez, Ana Sanfelix, Jan Balzarini, Erik De Clercq, Mariajose Camarasa
    Abstract:

    Several analogues of a new lead for anti-HIV-1 agents [1-[2',5'-bis-O-(Tert-Butyldimethylsilyl)-beta-D-ribofuranosyl]-thymine] -3'-spiro-5''-(4''-amino-1'',2''-oxathiole 2'',2''-dioxide) (TSAO) modified at positions N-3, O-4 and C-5 of the thymine moiety, have been prepared and evaluated as inhibitors of HIV-1 replication. A new stereoselective synthetic procedure is described. Reaction of 1,2-di-O-acetyl-5-O-benzoyl-3-C-cyano-3-O-mesyl-D-ribofuranose with pyrimidine bases, followed by treatment with Cs2CO3 afforded stereoselectively, beta-D-ribofuranosyl-3'-spiro nucleosides. 2',5'-O-Deacylation and subsequent treatment with Tert-Butyldimethylsilyl Chloride gave the TSAO derivatives. Only those analogues having a tBDMSi group at both the C-5' and C-2' positions of the ribose moiety showed potent anti-HIV-1 activity. The activity ranged from 0.060 microM to 1.0 microM. Introduction of an alkyl or alkenyl function at N-3 of the thymine ring markedly decreased cytotoxicity without affecting the antiviral activity. While markedly active against HIV-1, the TSAO derivatives had no activity against HIV-2 or SIV. They represent the first example of nucleoside analogues with an intact ribose moiety that discriminate between HIV-1 and other retroviruses.

Ana Sanfelix - One of the best experts on this subject based on the ideXlab platform.

  • tsao analogues stereospecific synthesis and anti hiv 1 activity of 1 2 5 bis o tert butyldimethylsilyl beta d ribofuranosyl 3 spiro 5 4 amino 1 2 oxathiole 2 2 dioxide pyrimidine and pyrimidine modified nucleosides
    Journal of Medicinal Chemistry, 1992
    Co-Authors: Mariajesus Perezperez, Ana Sanfelix, Jan Balzarini, Erik De Clercq, Mariajose Camarasa
    Abstract:

    Several analogues of a new lead for anti-HIV-1 agents [1-[2',5'-bis-O-(Tert-Butyldimethylsilyl)-beta-D-ribofuranosyl]-thymine] -3'-spiro-5''-(4''-amino-1'',2''-oxathiole 2'',2''-dioxide) (TSAO) modified at positions N-3, O-4 and C-5 of the thymine moiety, have been prepared and evaluated as inhibitors of HIV-1 replication. A new stereoselective synthetic procedure is described. Reaction of 1,2-di-O-acetyl-5-O-benzoyl-3-C-cyano-3-O-mesyl-D-ribofuranose with pyrimidine bases, followed by treatment with Cs2CO3 afforded stereoselectively, beta-D-ribofuranosyl-3'-spiro nucleosides. 2',5'-O-Deacylation and subsequent treatment with Tert-Butyldimethylsilyl Chloride gave the TSAO derivatives. Only those analogues having a tBDMSi group at both the C-5' and C-2' positions of the ribose moiety showed potent anti-HIV-1 activity. The activity ranged from 0.060 microM to 1.0 microM. Introduction of an alkyl or alkenyl function at N-3 of the thymine ring markedly decreased cytotoxicity without affecting the antiviral activity. While markedly active against HIV-1, the TSAO derivatives had no activity against HIV-2 or SIV. They represent the first example of nucleoside analogues with an intact ribose moiety that discriminate between HIV-1 and other retroviruses.

Jan Balzarini - One of the best experts on this subject based on the ideXlab platform.

  • tsao analogues stereospecific synthesis and anti hiv 1 activity of 1 2 5 bis o tert butyldimethylsilyl beta d ribofuranosyl 3 spiro 5 4 amino 1 2 oxathiole 2 2 dioxide pyrimidine and pyrimidine modified nucleosides
    Journal of Medicinal Chemistry, 1992
    Co-Authors: Mariajesus Perezperez, Ana Sanfelix, Jan Balzarini, Erik De Clercq, Mariajose Camarasa
    Abstract:

    Several analogues of a new lead for anti-HIV-1 agents [1-[2',5'-bis-O-(Tert-Butyldimethylsilyl)-beta-D-ribofuranosyl]-thymine] -3'-spiro-5''-(4''-amino-1'',2''-oxathiole 2'',2''-dioxide) (TSAO) modified at positions N-3, O-4 and C-5 of the thymine moiety, have been prepared and evaluated as inhibitors of HIV-1 replication. A new stereoselective synthetic procedure is described. Reaction of 1,2-di-O-acetyl-5-O-benzoyl-3-C-cyano-3-O-mesyl-D-ribofuranose with pyrimidine bases, followed by treatment with Cs2CO3 afforded stereoselectively, beta-D-ribofuranosyl-3'-spiro nucleosides. 2',5'-O-Deacylation and subsequent treatment with Tert-Butyldimethylsilyl Chloride gave the TSAO derivatives. Only those analogues having a tBDMSi group at both the C-5' and C-2' positions of the ribose moiety showed potent anti-HIV-1 activity. The activity ranged from 0.060 microM to 1.0 microM. Introduction of an alkyl or alkenyl function at N-3 of the thymine ring markedly decreased cytotoxicity without affecting the antiviral activity. While markedly active against HIV-1, the TSAO derivatives had no activity against HIV-2 or SIV. They represent the first example of nucleoside analogues with an intact ribose moiety that discriminate between HIV-1 and other retroviruses.

Erik De Clercq - One of the best experts on this subject based on the ideXlab platform.

  • tsao analogues stereospecific synthesis and anti hiv 1 activity of 1 2 5 bis o tert butyldimethylsilyl beta d ribofuranosyl 3 spiro 5 4 amino 1 2 oxathiole 2 2 dioxide pyrimidine and pyrimidine modified nucleosides
    Journal of Medicinal Chemistry, 1992
    Co-Authors: Mariajesus Perezperez, Ana Sanfelix, Jan Balzarini, Erik De Clercq, Mariajose Camarasa
    Abstract:

    Several analogues of a new lead for anti-HIV-1 agents [1-[2',5'-bis-O-(Tert-Butyldimethylsilyl)-beta-D-ribofuranosyl]-thymine] -3'-spiro-5''-(4''-amino-1'',2''-oxathiole 2'',2''-dioxide) (TSAO) modified at positions N-3, O-4 and C-5 of the thymine moiety, have been prepared and evaluated as inhibitors of HIV-1 replication. A new stereoselective synthetic procedure is described. Reaction of 1,2-di-O-acetyl-5-O-benzoyl-3-C-cyano-3-O-mesyl-D-ribofuranose with pyrimidine bases, followed by treatment with Cs2CO3 afforded stereoselectively, beta-D-ribofuranosyl-3'-spiro nucleosides. 2',5'-O-Deacylation and subsequent treatment with Tert-Butyldimethylsilyl Chloride gave the TSAO derivatives. Only those analogues having a tBDMSi group at both the C-5' and C-2' positions of the ribose moiety showed potent anti-HIV-1 activity. The activity ranged from 0.060 microM to 1.0 microM. Introduction of an alkyl or alkenyl function at N-3 of the thymine ring markedly decreased cytotoxicity without affecting the antiviral activity. While markedly active against HIV-1, the TSAO derivatives had no activity against HIV-2 or SIV. They represent the first example of nucleoside analogues with an intact ribose moiety that discriminate between HIV-1 and other retroviruses.