Stereoselective synthesis of the hydroxyethylene isostere of the HIV protease (Tyr-Pro) cleavage site

The stereoselective, syntheses and IC 50's of Tyr-HE-Pro based inhibitors are reported. The [2S,3S,4S,5S]-stereochemistry was preferred by HIV-1 protease. The stereoselective syntheses and IC 50's of Tyr-HE-Pro based inhibitors ( 15) via intramolecular epoxide alkylation of 10 are reported...

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Veröffentlicht in:Tetrahedron letters 1992-05, Vol.33 (21), p.2957-2960
Hauptverfasser: Thompson, Wayne J., Ball, Richard G., Darke, Paul L., Zugay, Joan A., Thies, J.E.
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Sprache:eng
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Zusammenfassung:The stereoselective, syntheses and IC 50's of Tyr-HE-Pro based inhibitors are reported. The [2S,3S,4S,5S]-stereochemistry was preferred by HIV-1 protease. The stereoselective syntheses and IC 50's of Tyr-HE-Pro based inhibitors ( 15) via intramolecular epoxide alkylation of 10 are reported.
ISSN:0040-4039
1873-3581
DOI:10.1016/S0040-4039(00)79571-2